Synthesis of Novel Ethyl (substituted)phenyl‐4‐oxothiazolidin‐3‐yl)‐1‐ethyl‐4‐oxo‐1,4‐dihydroquinoline‐3‐Carboxylates as Potential Anticancer Agents

A series of ethyl (substituted)phenyl‐4‐oxothiazolidin‐3‐yl)‐1‐ethyl‐4‐oxo‐1,4‐dihydroquinoline‐3‐carboxylates ( 7a , 7b , 7c , 7d , 7e , 7f , 7g ) has been prepared from reactions between aminoquinolones 6 with arenealdehydes and mercaptoacetic acid. The critical intermediates, 6 a and 6b , were obtained from appropriate amines by a sequence of steps involving (i) reaction with diethylethoxymethylenemalonate, (ii) thermal cyclization in diphenyl ether, (iii) ethylation and (iv) Pd/C catalyzed reduction. New compounds 7a , 7b , 7c , 7d , 7e , 7f , 7g were fully identified and characterized by NMR (¹H and ¹³C) and specifically for 7d by X‐ray crystallography. Compounds 7b , 7c , 7d , 7e , 7f were found not to exhibit activity at 10 uM concentrations against gastric ascitis (AGP‐01), gastric adenocarcinoma kind intestinal (ACP‐02), colon (HCT‐116) and murine melanome (B16F10) cancer cells. However, none exhibited cytotoxicity against normal cells human fibroblast (MRC‐5), murine fibroblast (NIH3T3) and normal human melanocyte (Melan‐A).     

Synthesis of 11-hydroxydrim-8(9)-en-7-one and 11,12-dihydroxydrim-8(9)-en-7-one from drim-8(9)-en-7-one

A synthetic route to 11-hydroxydrim-8(9)-en-7-one and 11,12-hydroxydrim-8(9)-en-7-one, valuable key intermediates for the preparation of naturally occurring biologically active drimanic sesquiterpenoids, starting from easily available drim-8(9)-en-7-one was developed. 11-Hydroxydrim-8(9)-en-7-one was obtained by peracidic oxidation of the enol acetate of drim-8(9)-en-7-one. 11,12-Dihydroxydrim-8(9)-en-7-one was synthesized from drim-8(9)-en-7-one by two routes, namely, by a five-step procedurevia 11-hydroxydrim-8(9)-en-7-one and by bromination of drim-8(9)-en-7-one with NBS to give 11,12-dibromodrim-8(9)-en-7-one followed by its acetoxylation and deacetylation. Deceased Translated fromIzvestiya Akademii Nauk, Seriya Khimicheskaya, No. 1, pp. 95–98, January, 2000.     

A slipped multi-decker zirconium complex with an η7:η2-bridging cycloheptatrienyl ligand

The complex [(η(7)-C(7)H(7))Zr{N(SiMe(3))(2)}(thf)] (2) loses THF upon sublimation to afford a chain polymer consisting of [(η(7)-C(7)H(7))Zr{N(SiMe(3))(2)}] (3) units; they are connected by cycloheptatrienyl ligands in an unprecedented antifacial η(7):η(2)-bridging mode. The basicity of the bis(trimethylsilyl)amido ligand can also be used to introduce other ligands by acid-base reactions.     

Synthesis of 11-hydroxydrim-8(9)-en-7-one and 11,12-dihydroxydrim-8(9)-en-7-one from drim-8(9)-en-7-one

A synthetic route to 11-hydroxydrim-8(9)-en-7-one and 11,12-hydroxydrim-8(9)-en-7-one, valuable key intermediates for the preparation of naturally occurring biologically active drimanic sesquiterpenoids, starting from easily available drim-8(9)-en-7-one was developed. 11-Hydroxydrim-8(9)-en-7-one was obtained by peracidic oxidation of the enol acetate of drim-8(9)-en-7-one. 11,12-Dihydroxydrim-8(9)-en-7-one was synthesized from drim-8(9)-en-7-one by two routes, namely, by a five-step procedurevia 11-hydroxydrim-8(9)-en-7-one and by bromination of drim-8(9)-en-7-one with NBS to give 11,12-dibromodrim-8(9)-en-7-one followed by its acetoxylation and deacetylation. Deceased Translated fromIzvestiya Akademii Nauk, Seriya Khimicheskaya, No. 1, pp. 95–98, January, 2000.     

Diisophorone and related compounds—II: 1-Alkoxy- and 1-carboxy-diisophorane derivatives

The acid catalysed interaction in dioxan of trialkyl orthoformates with diisophor-2(7)-en-ol-3-one, diisophor-2(7)-en-ol, and their bisnor-homologues, provides the corresponding 1-alkoxy-compounds. Their structure is established by the identity of -methoxydiisophor-2(7)-en-3-one obtained by this method, and by the action of sodium methoxide on 1-chlorodiisophor-2(17)-en-3-one. The latter is regenerated from 1-methoxy(or ethoxy) diisophor-2(7)-en-3-one by the action of stannic chloride-acetyl chloride. Catalytic hydrogenation reduces the 3-keto-function in 1-alkoxydiisophor-2(7)-en-3-ones to a methylene unit; simultaneous removal of the 1-alkoxy-group in the case of the 1-isopropoxy-homologue yields the penultimate parent hydrocarbon of this series, diisophor-2(7)-ene.The combined action of silver sulphate and formic acid in concentrated sulphuric acid on 1-chlorodiisophor-2(7)-en-3-one (and its bisnor-homologue) produces the corresponding 1-carboxylic acids. These are also obtainable by the hydrolysis of the 1-cyano-compound, and are esterifiable by the standard methods.     

Synthesis and Antimicrobial Activities of Novel Series of 3‐(4‐(2‐substituted thiazol‐4‐yl)phenyl)‐2‐(4‐methyl‐2‐substituted thiazol‐5‐yl)thiazolidin‐4‐one Derivatives

In the present investigation, a novel series of 3‐(4‐(2‐substituted thiazol‐4‐yl)phenyl)‐2‐(4‐methyl‐2‐substituted thiazol‐5‐yl)thiazolidin‐4‐one derivatives were synthesized by condensation of 2‐substituted‐4‐methylthiazole‐5‐carbaldehyde with 4‐(2‐substituted thiazol‐4‐yl)benzenamine followed by cyclo‐condensation with thioglycolic acid in toluene. All the newly synthesized compounds were characterized by spectral (IR, ¹H NMR, ¹³C NMR, and Mass) methods. The title compounds were screened for quantitative antibacterial activity (minimal inhibitory concentration). All compounds 7a , 7b , 7c , 7d , 7e , 7f , 7g , 7h and 8a , 8b , 8c , 8d , 8e , 8f , 8g , 8h show moderate to good antimicrobial activity, whereas compounds ( 7a , 7b , 7c , 7d , 7e , 7f , 7g , 7h ) also show moderate antifungal activity.     

C---H bond activation by rhodium(I) and the mechanism of the olefin isomerization: new synthesis of β,γ-unsaturated ketones via η- or η-alkylallylrhodium(III) complexes by reductive elimination

Acylrhodium(III)-η³-1-ethylallyl complex (7) was prepared by the reaction of 8-quinolinecarboxaldehyde (3) and 1,4-pentadienerhodium(I) chloride (2) by C---H bond activation, followed by hydrometallation, and double bond migration. Higher concentrations of pyridine as coordinating ligand transforms η³-1-ethylallylrhodium(III) complexes (8a,8b) into η¹-pent-2-enylrhodium(III) complex (11a). Acylrhodium(III)-η³-syn,anti-1,3-dimethylallyl complex (14) was also prepared from 1,3-pentadienerhodium(I) chloride (16) and 3. The reductive elimination of acylrhodium(III)-η¹- and -η³-1-alkylallyl complexes by trimethylphosphite gives various β,γ-unsaturated ketones.     

Equilibrium geometries and associated energetic properties of mixed metal-silicon clusters from global optimization

The structural properties of the cluster series Me(m)Si(7-m) (Me = Cu and Li, m < or = 6) are studied by density functional theory (DFT) employing a plane wave basis. The equilibrium geometries and energetic properties of these clusters are obtained by use of the simulated annealing procedure in conjunction with the Nosé thermostat algorithm. The lowest energy isomer thus obtained is analyzed by density functional theory at the B3LYP/6-311+G(d,p) level including all electrons. Pentagonal ground state structures derived from the D(5)(h) equilibrium geometries of both Si(7) and Cu(7) are obtained for Cu(m)Si(7-m) with m < 6. The Li(m)Si(7-m) clusters, in contrast, tend toward adsorption geometries where m Li atoms are attached to a Si(7-m)framework with pronounced negative charge. For both Li(m)Si(7-m) and Cu(m)Si(7-m), a marked decrease of the energy gap is found as the number of metal atom constituents increases.     

Derivatives of 1,5-diamino-1H-tetrazole: a new family of energetic heterocyclic-based salts

1,5-Diamino-1H-tetrazole (2, DAT) can easily be protonated by reaction with strong mineral acids, yielding the poorly investigated 1,5-diaminotetrazolium nitrate (2a) and perchlorate (2b). A new synthesis for 2 is introduced that avoids lead azide as a hazardous byproduct. The reaction of 1,5-diamino-1H-tetrazole with iodomethane (7a) followed by the metathesis of the iodide (7a) with silver nitrate (7b), silver dinitramide (7c), or silver azide (7d) leads to a new family of heterocyclic-based salts. In all cases, stable salts were obtained and fully characterized by vibrational (IR, Raman) spectroscopy, multinuclear NMR spectroscopy, mass spectrometry, elemental analysis, X-ray structure determination, and initial safety testing (impact and friction sensitivity). Most of the salts exhibit good thermal stabilities, and both the perchlorate (2b) and the dinitramide (7c) have melting points well below 100 degrees C, yet high decomposition onsets, defining them as new (7c), highly energetic ionic liquids. Preliminary sensitivity testing of the crystalline compounds indicates rather low impact sensitivities for all compounds, the highest being that of the perchlorate (2b) and the dinitramide (7c) with a value of 7 J. In contrast, the friction sensitivities of the perchlorate (2b, 60 N) and the dinitramide (7c, 24 N) are relatively high. The enthalpies of combustion (Delta(c)H degrees ) of 7b-d were determined experimentally using oxygen bomb calorimetry: Delta(c)H degrees (7b) = -2456 cal g(-)(1), Delta(c)H degrees (7c) = -2135 cal g(-)(1), and Delta(c)H degrees (7d) = -3594 cal g(-)(1). The standard enthalpies of formation (Delta(f)H degrees ) of 7b-d were obtained on the basis of quantum chemical computations using the G2 (G3) method: Delta(f)H degrees (7b) = 41.7 (41.2) kcal mol(-)(1), Delta(f)H degrees (7c) = 92.1 (91.1) kcal mol(-)(1), and Delta(f)H degrees (7d) = 161.6 (161.5) kcal mol(-)(1). The detonation velocities (D) and detonation pressures (P) of 2b and 7b-d were calculated using the empirical equations of Kamlet and Jacobs: D(2b) = 8383 m s(-)(1), P(2b) = 32.2 GPa; D(7b) = 7682 m s(-)(1), P(7b) = 23.4 GPa; D(7c) = 8827 m s(-)(1), P(7c) = 33.6 GPa; and D(7d) = 7405 m s(-)(1), P(7d) = 20.8 GPa. For all compounds, a structure determination by single-crystal X-ray diffraction was performed. 2a and 2b crystallize in the monoclinic space groups C2/c and P2(1)/n, respectively. The salts of 7 crystallize in the orthorhombic space groups Pna2(1) (7a, 7d) and Fdd2 (7b). The hydrogen-bonded ring motifs are discussed in the formalism of graph-set analysis of hydrogen-bond patterns and compared in the case of 2a, 2b, and 7b.     

Investigation of hydrogen absorption in Li7VN4 and Li7MnN4

The hydrogen storage properties of Li(7)VN(4) and Li(7)MnN(4) were investigated both by experiment and by density functional theory calculations. Li(7)VN(4) did not sorb hydrogen under our experimental conditions. Li(7)MnN(4) was observed to sorb 7 hydrogen atoms through the formation of LiH, Mn(4)N, and ammonia gas. An applied pressurized mixture of H(2)/Ar and H(2)/N(2) gases was helpful to mitigate the release of NH(3) but could not prevent its formation. The introduction of N(2) also caused weight gain of the sample by re-nitriding the absorbed products LiH and Mn(4)N, which correlated with the presence of Li(2)NH, LiNH(2), and Mn(2)N detected by X-ray diffraction. While our observed results for Li(7)VN(4) and Li(7)MnN(4) differ in detail, they are in overall qualitative agreement with our theoretical work, which strongly suggests that both compounds are unlikely to form quaternary hydrides.     

Syntheses,structures and properties of five chiral quaternary sulfides,AlxLn_3(Si_yAl_(1-γ))S_7 (Ln=Y,Gd,Dy) and In_(0.33)Sm_3SiS_7

Five new quaternary isostructural rare-earth sulfides, Al0.57Gd3(Si0.27Al0.73)S7 (1), Al0.55Dy3(Si0.34Al0.66)S7 (2), Al0.50Y3(Si0.50Al0.50)S7 (3), Al0.44Gd3(Si0.70Al0.30)S7 (4) and In0.33Sm3SiS7 (5), have been synthesized by facile solid-state reactions. They crystallize in the 3-D ALn3EQ7 structure type in the hexagonal chiral space group P63. The structures feature a 3-D host framework constructed by Ln-S bicapped trigonal prisms, in which the octahedral and tetrahedral interspaces are occupied by A and E...     

Synthesis of derivatives of 7-iodo-4-aminoquinolines

7-Iodo- and 7,8-diiodo-4-(3-dimethylaminopropylamino)quinolines and 7-iodo-4-(3) dipropyl-aminopropylamlno)- and 7-iodo-4-(3-diallylaminopropylamino)quinoline were obtained by the reaction of 7-iodo- and 7,8-diodo-4-chloroquinolines with the corresponding diamines. The catalytic hydrogenation of 7-iodo-4-(3-diallylaminopropylamino)quinoline at normal pressure leads to 7-iodo-4-(3-dipropylaminopropylamino)quinoline.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 972–975, July, 1980.     

Comparative Structural Study of Three Tetrahalophthalic Anhydrides: Recognition of X···O(anhydride) Halogen Bond and πh···O(anhydride) Interaction

Structures of three tetrahalophthalic anhydrides (TXPA: halogen = Cl (TCPA), Br (TBPA), I (TIPA)) were studied by X-ray diffraction, and several types of halogen bonds (HaB) and lone pair···π-hole (lp···πh) contacts were revealed in their structures. HaBs involving the central oxygen atom of anhydride group (further X···O(anhydride) were recognized in the structures of TCPA and TBPA. In contrast, for the O(anhydride) atom of TIPA, only interactions with the π system (π-hole) of the anhydride ring (further lp(O)···πh) were observed. Computational studies by a number of theoretical methods (molecular electrostatic potentials, the quantum theory of atoms in molecules, the independent gradient model, natural bond orbital analyses, the electron density difference, and symmetry-adapted perturbation theory) demonstrated that the X···O(anhydride) contacts in TCPA and TBPA and lp(O)···πh in TIPA are caused by the packing effect. The supramolecular architecture of isostructural TCPA and TBPA was mainly affected by X···O(acyl) and X···X HaBs, and, for TIPA, the main contribution provided I···I HaBs.     

Benzo‐Fused Double [7]Carbohelicene: Synthesis,Structures, and Physicochemical Properties

A benzo‐fused double [7]carbohelicene (D7H) was synthesized through a regioselective cyclodehydrogenation of a tetranaphthyl‐p ‐terphenyl‐based precursor. The twisted (D7H‐1) and anti ‐folded (D7H‐2) conformers of D7H were separated by recrystallization, and their double helicene structures with overlapping terminal benzene rings were unambiguously elucidated by X‐ray crystallography. A record‐high isomerization barrier (46.0 kcal mol⁻¹) in double helicenes was estimated based on density functional theory (DFT) calculation, which resulted in the excellent conformational stability of D7H. The physicochemical properties of D7H‐1 and D7H‐2 were investigated by UV/Vis absorption spectroscopy and cyclic voltammetry, displaying the variation of electronic structure upon conformational changes. The optical resolution of the racemic D7H‐1 was carried out by chiral HPLC, offering enantiopure D7H‐1‐(P ,P ) and D7H‐1‐(M ,M ), which were further characterized by circular dichroism spectroscopy.     

Synthesis and crystal structure of the complex [MoW(OEt)(μ-CH2){μ-C(C6H4Me-4)C(Me)O}(η-C7H7)(η-C2B9H10Me)]

The complex [MoW(μ-CC₆H₄Me-4)(CO)₂(η⁷-C₇H₇)(η⁵-C₂B₉H₁₀Me)] reacts with diazomethane in Et₂O containing EtOH to afford the dimetal compound [MoW(OEt)(μ-CH₂){μ-C(C₆H₄Me-4)C(Me)O}(η⁷-C₇H₇)(η⁵-C₂B₉H₁₀Me)]. The structure of this product was established by X-ray diffraction. The Mo---W bond [2.778(4) Å] is bridged by a CH₂ group [μ-C---Mo 2.14(3), μ-C---W 2.02(3) Å] and by a C(C₆H₄Me-4)C(Me)O fragment [Mo---O 2.11(3), W---O 2.18(2), Mo---C(C₆H₄Me-4) 2.41(3), W---C(C₆H₄Me-4) 2.09(3), Mo---C(Me) 2.26(3) Å]. The molybdenum atom is η⁷-coordinated by the C₇H₇ ring and the tungsten atom is η⁵-coordinated by the open pentagonal face of the nido-icosahedral C₂B₉H₁₀Me cage. The tungsten atom also carries a terminally bound OEt group [W---O 1.88(3) Å]. The ¹H and ¹³C-{¹H} NMR data for the dimetal compound are reported and discussed.     

A fragmentation study of a flavone triglycoside, kaempferol-3-O-robinoside-7-O-rhamnoside

A mass spectrometric method based on the combined use of electrospray ionization, collision-induced dissociation and tandem mass spectrometry has been applied to the structural characterization of the flavone triglycoside, robinin (3,5,7,4'-tetrahydroxyflavone-3-O-robinoside-7-O-rhamnoside). The deprotonated molecule fragments by loss of the rhamnose glycan residue to yield the Y(7) (-) ion (m/z 593) and by scission of the robinose glycan residue to yield the radical anion [Y(3,0)-H](-.) (m/z 430). The Y(7) (-) ion fragments by scission of the robinose glycan residue to yield the radical anion of Y(7)[Y(3,0)-H](-.) (m/z 284). The [Y(3,0)-H](-.) radical anion fragments by loss of the rhamnose glycan residue to yield the radical anion Y(7)[Y(3,0)-H](-.) (m/z 284) and by scission to yield [Y(7)-H][Y(3,0)--H](-) (m/z 283). A fragmentation mechanism has been proposed.     

天然黄酮香叶木素类及其衍生物的合成与生物活性研究

以橙皮苷为原料,经脱氢、选择性甲基化、糖苷水解、相转移催化下的糖苷化反应、异戊烯基化和法呢烯基化等反应步骤,分别合成了3’-O-甲基香叶木素(1),香叶木素-7-O-β-D-葡萄糖苷(2),香叶木素-7-O-β-D-半乳糖苷(3),3’-O-甲基香叶木素-7-O-β-D-葡萄糖苷(4)4种天然产物及3’-O-甲基香叶木素-7-O-β-D-半乳糖苷(5),香叶木素-7-O-β-D-乙酰葡萄糖苷(6)、香叶木素-7-O-β-D-乙酰半乳糖苷(7),3’-O-甲基香叶木素-7-O-β-D-乙酰葡萄糖苷(8),3’-O-甲基香叶木素-7-O-β-D-乙酰半乳糖苷(9),7-O-异戊基香叶木素(10),7-O-异戊烯基-3’-O-甲基香叶木素(11)和7-O-法呢烯基-3’-O-甲基香叶木素(12)8种新的香叶木素衍生物.所合成化合物的结构已由核磁共振谱、红外光谱和质谱所证实,并用比色法MTT[3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐]蛋白染色法对所合成的目标化合物进行了体外抗肿瘤细胞生物活性测试,发现化合物6,10和11对肝癌细胞(SMMC-7721)、乳腺癌细胞(MCF-7)和结肠癌细胞(SW480)有一定的抑制活性.     

Activation energies for dissociation of double strand oligonucleotide anions: evidence for watson-crick base pairing in vacuo

The dissociation kinetics of a series of complementary and noncomplementary DNA duplexes, (TGCA)(2) (3-), (CCGG)(2) (3-), (AATTAAT)(2) (3-), (CCGGCCG)(2) (3-), A(7).T(7) (3-), A(7).A(7) (3-), T(7).T(7) (3-), and A(7).C(7) (3-) were investigated using blackbody infrared radiative dissociation in a Fourier transform mass spectrometer. From the temperature dependence of the unimolecular dissociation rate constants, Arrhenius activation parameters in the zero-pressure limit are obtained. Activation energies range from 1.2 to 1.7 eV, and preexponential factors range from 10(13) to 10(19) s(-1). Dissociation of the duplexes results in cleavage of the noncovalent bonds and/or cleavage of covalent bonds leading to loss of a neutral nucleobase followed by backbone cleavage producing sequence-specific (a - base) and w ions. Four pieces of evidence are presented which indicate that Watson-Crick (WC) base pairing is preserved in complementary DNA duplexes in the gas phase: i. the activation energy for dissociation of the complementary dimer, A(7).T(7) (3-), to the single strands is significantly higher than that for the related noncomplementary A(7).A(7) (3-) and T(7).T(7) (3-) dimers, indicating a stronger interaction between strands with a specific base sequence, ii. extensive loss of neutral adenine occurs for A(7).A(7) (3-) and A(7).C(7) (3-) but not for A(7).T(7) (3-) consistent with this process being shut down by WC hydrogen bonding, iii. a correlation is observed between the measured activation energy for dissociation to single strands and the dimerization enthalpy (-DeltaH(d)) in solution, and iv. molecular dynamics carried out at 300 and 400 K indicate that WC base pairing is preserved for A(7).T(7) (3-) duplex, although the helical structure is essentially lost. In combination, these results provide strong evidence that WC base pairing can exist in the complete absence of solvent.     

An amidinate-stabilized germatrisilacyclobutadiene ylide

The synthesis and characterization of new amidinate-stabilized germatrisilacyclobutadiene ylides [L(3)Si(3)GeL'] (L=PhC(NtBu)(2); L'=?L; ?=Ge (3), Si (7)) are described. Compound 3 was prepared by the reaction of [LSi-SiL] (1) with one equivalent of [LGe-GeL] (2) in THF. Compound 7 was synthesized by the reaction of 2 with excess 1 in THF. The bisamidinate germylene [L(2)Ge:] (4) is a by-product in both reactions. Moreover, compound 7 was prepared by the reaction of 3 with one equivalent of 1 in THF. Compounds 3 and 7 have been characterized by NMR spectroscopy, X-ray crystallography, and theoretical studies. The results show that compounds 3 and 7 are not antiaromatic. The puckered Si(3) Ge four-membered rings in 3 and 7 have a ylide structure, which is stabilized by amidinate ligands and the electron delocalization within the Si(3) Ge four-membered ring.     

Grinding and Microwave‐assisted Synthesis of Heterocyclic Molecules in High Yields and Their Biological Evaluation

Cis‐cyclohexane1,2‐dicarboxylic acid ( 1a ), phthalic acid ( 1b ), and pyrazine 2,3‐ dicarboxylic acid ( 1c ) on grinding with hydrazine hydrate ( 2a ) gave 2‐aminohexahydro‐1H‐isoindole‐1,3(2H)‐dione ( 3a ), 2‐amino‐1H‐isoindole‐1,3(2H)‐dione ( 3b ), and 6‐amino‐5H‐pyrrolo[3,4‐b]pyrazine‐5,7(6H)‐dione ( 3c ), respectively. Condensation of ( 3a , 3b , 3c ) with aldehydes ( 4x , 4y , 4z ) and 2‐cyanopyridine, 4‐cyanopyridine, 2‐cyanopyrazine ( 5x , 5y , 5z ) under microwave irradiation gave corresponding azomethine ( 6ax , 6ay , 6az , 6bx , 6by , 6bz , 6cx , 6cy , 6cz ) and amidine ( 7ax , 7ay , 7az , 7bx , 7by , 7bz , 7cx , 7cy , 7cz ) derivatives, respectively. Fully characterized azomethine ( 6ax , 6ay , 6az , 6bx , 6by , 6bz , 6cx , 6cy , 6cz ) and amidine ( 7ax , 7ay , 7az , 7bx , 7by , 7bz , 7cx , 7cy , 7cz ) derivatives were screened for anti‐inflammatory and anticancer activity against five human cancer cell lines. Compound 7cx exhibited 35% anti‐inflammatory activity at a dose of 50 mg/kg p.o. whereas standard drug ibuprofen showed 39% activity at a dose of 50 mg/kg p.o. Compounds 6bz , 7cx , 7cz (breast T47D), 6bz , 6cy (lung NCI H‐522), 6bx , 7bz (colon HCT‐15), 6bz (ovary PA‐1) and 6bx , and 6cz (liver HepG‐2) exhibited good (35–41% inhibition at 10 μM c) anticancer activity. IC₅₀ values of 6bx , 6bz , 6cy , 6cz , 7bz , 7cx , and 7cz against various cancer cell lines and normal cell (COS‐1) are also reported.