共查询到20条相似文献,搜索用时 15 毫秒
1.
Novel Pyrimidine‐based Ferrocenyl substituted Organometallic Compounds: Synthesis,Characterization and Biological Evaluation 下载免费PDF全文
Humaira Parveen Meshari A. Alsharif Mohammed I. Alahmdi Sayeed Mukhtar Amir Azam 《应用有机金属化学》2018,32(4)
Some novel pyrimidine‐based ferrocenyl substituted organometallic compounds were synthesized via multistep reactions, well characterized by different spectroscopic techniques and elemental analyses and evaluated for in vitro antiprotozoal susceptibility against HM1: IMSS strain of Entamoeba histolytica. The results of antiprotozoal susceptibility unveiled these compounds, as new leads in protozoal chemotherapy as most of the organometallics displayed an exceptionally higher antiamoebic activity (IC50 = 0.055 μM ‐ 0.815 μM) than the reference drug metronidazole which gave IC50 (50% inhibitory concentration) value 1.781 μM in our experiments, concluding that newly synthesized organometallic compounds have potential to be employed as effective antiamoebic agents and these organometallics can be very useful for further optimization work on amoebic chemotherapy. 相似文献
2.
Srinivas Endoori Kali Charan Gulipalli Srinu Bodige Parameshwar Ravula Nareshvarma Seelam 《Journal of heterocyclic chemistry》2021,58(6):1311-1320
A novel series of imidazo[1,2-a]pyridine based 1H-1,2,3-triazole derivatives were designed, synthesized, and evaluated for their anticancer activity against two different human cancer cell lines. Most of the synthesized compounds displayed anticancer activity with IC50 values from 2.35 to 120.46 μM. Furthermore, compounds 9b , 9c, 9d, 9f , and 9j showed potent inhibitory activity against cancer cell lines, with IC50 values close to that of standard drug. It is important to note that compound 9d was more potent than the standard drug cisplatin with IC50 values of 10.89 and 2.35 μM against Hela cell line and MCF-7 cell line, respectively. 相似文献
3.
K Benci L Mandić T Suhina M Sedić M Klobučar S Kraljević Pavelić K Pavelić K Wittine M Mintas 《Molecules (Basel, Switzerland)》2012,17(9):11010-11025
We report here on the synthesis and in vitro anti-tumor effects of a series of novel 1,2,4-triazole (compounds 3-6), 4,5-dicyanoimidazole (compound 7), and purine (compounds 8-13) coumarin derivatives and their acyclic nucleoside analogues 14-18. Structures of novel compounds 3-18 were deduced from their 1H- and 13C-NMR and corresponding mass spectra. Results of anti-proliferative assays performed on a panel of selected human tumor cell lines revealed that compound 6 had moderate cytostatic activity against the HeLa cell line (IC50 = 35 μM), whereas compound 10 showed moderate activity against the HeLa (IC50 = 33 μM), HepG2 (IC50 = 25 μM) and SW620 (IC50 = 35 μM) cell lines. These compounds showed no cytotoxic effects on normal (diploid) human fibroblasts. 相似文献
4.
Nagaraju Chirra Varshitha Shanigarapu Naga Pranathi Abburi Ekaterina O. Sinegubova Ravi Kumar Pedapati Yana L. Esaulkova Vladimir V. Zarubaev Srinivas Kantevari 《Journal of heterocyclic chemistry》2024,61(3):496-505
Herein described the synthesis and antiviral evaluation of a novel series of morpholine and thio-morpholine coupled imidazo[2,1-b]thiazoles. The three-step reaction sequence involving the condensation of 1,3-dichloroacetone with thiourea followed by coupling with morpholine and thiomorpholine and finally cyclization with substituted α-bromoacetophenones yielded the desired imidazothiazoles 7(a–l) . Screening of all the new compounds for their in vitro antiviral activity against influenza virus A/Puerto Rico/8/34 (H1N1) in MDCK cells, resulted in two potent analogs, 7d (IC50: 1.1 μM, C50: >300 μM, SI = 273) and 7e (IC50: 2.0 μM, C50: >300 μM, SI = 150), with a favorable toxicity profile and are the best anti-influenza hit analogs for further structural optimization. 相似文献
5.
In this work, peripheral or nonperipheral tetra‐[4‐(9H‐carbazol‐9‐yl)phenoxy] substituted cobalt(II), manganese (III) phthalocyanines were synthesized for the first time. Their acetylcholinesterase from Electrophorus electricus (AChE), butyrylcholinesterase equine serum (BuChE), and α‐glucosidase Saccharomyces cerevisiae inhibition were investigated spectrophotometrically. Finally, in vitro cytotoxicities of the compounds were investigated on human neuroblastoma (SH‐SY5Y) cell line using MTT cell viability assay. The compounds inhibited to enzymes in the range of 7.39 ± 0.25–35.29 ± 2.49 μM with IC50 values for AChE and 14.38 ± 0.66–58.02 ± 4.94 μM for BuChE as compared with galantamine, which used as a positive control. For α‐glucosidase, all compounds had stronger inhibition action than acarbose according to the IC50 values. The IC50 values of N? Co and N? Mn were found to be 3.05 ± 0.10 and 15.82 ± 1.85 μM, respectively. The results of cytotoxicity showed that the IC50 values were above 100 μM showing the compounds had low cytotoxic action against SH‐SY5Y cell line for 24 h. Overall, carbazole substituted nonperipheral compounds can be considered as a potential agent for the treatment of Alzheimer's diseases and diabetes mellitus. 相似文献
6.
Maryam Mohammadi-Khanaposhtani Hoda Yahyavi Somaye Imanparast Fereshte Nazemi Harandi Mohammad Ali Faramarzi Alireza Foroumadi Bagher Larijani Mahmood Biglar Mohammad Mahdavi 《中国化学会会志》2020,67(5):856-863
Benzoylquinazolinone derivatives 3a–n were synthesized via a simple one-step reaction, and evaluated for in vitro α-glucosidase inhibitory activity. Compounds 3d , 3f–g , 3i , and 3m–n showed more inhibitory activity than standard drug acarbose (IC50 = 750.0 ± 1.5 μM), and among them, compound 3d displayed the highest α-glucosidase inhibitory activity (IC50 = 261.6 ± 0.1 μM). The kinetic analysis of the compound 3d revealed that this compound inhibited α-glucosidase in a competitive manner (Ki = 255 μM). The docking studies were applied to predict binding modes of the synthesized compounds in active site of α-glucosidase. 相似文献
7.
Cem Yamali Feyza Sena Engin Sinan Bilginer Mehtap Tugrak Dilan Ozmen Ozgun Gulsen Ozli Serkan Levent Begum Nurpelin Saglik Yusuf Ozkay Halise Inci Gul 《Journal of heterocyclic chemistry》2021,58(1):161-171
Chalcones targeting neurodegenerative diseases have been known as attractive structures in drug design and discovery. In this study, phenothiazine-based chalcones as ChEs and MAOs inhibitors were designed and synthesized via base-catalyzed Claisen-Schmidt condensation, and chemical structures of the compounds were elucidated by NMRs and HRMS. Compounds 3 and 9 showed promising inhibition potency against AChE enzyme with IC50 values of 0.221 μM and 0.053 μM while compound 9 displayed remarkable inhibition potency toward MAO-B enzyme with IC50 value of 0.048 μM. Compound 9 , as a dual-target inhibitor, selectively inhibited AChE and MAO-B enzymes. This promising behavior is an advantage for the compound since MAO-B and AChE inhibition have a role in Alzheimer's disease. Fused tricyclic ring systems such as phenothiazine incorporated with chalcone moiety being multitargeting ligands may help scientists for the rational design of novel lead compounds targeting neurodegenerative illnesses. 相似文献
8.
Qiujing Li Guijun Liu Ningning Wang Huiyong Yin Zhulai Li 《Journal of heterocyclic chemistry》2020,57(3):1220-1227
A series of benzotriazole (BTA) derivatives were synthesized as tyrosine protein kinase inhibitors using fragment-based design strategy. All desired compounds were synthesized with the reaction of benzotriazole, chloroacetonitrile and aromatic aldehyde using Ultrasonic-Microwave method and characterized by IR, 1H and 13C-NMR, mass spectrometry (MS) and elemental analysis. The anticancer activity of these compounds was evaluated by CCK-8 method against carcinoma VX2, lung cancer A549, stomach cancer cell lines MKN45 and MGC in vitro. The results showed that all compounds showed good antiproliferative activity. In particular, compound 2.1 showed the most prominent inhibition of VX2 cell lines with IC50 of 3.80 ± 0.75 μM. Compound 2.2 exhibited highly potent anticancer activity of stomach MGC cell lines with IC50 of 3.72 ± 0.11 μM. A549 and MKN45 cell lines were sensitive to compound 2.5 with IC50 of 5.47 ± 1.11 and 3.04 ± 0.02 μM, respectively. 相似文献
9.
Stefan Peterli Dieter Hubmann Urs Squin Helmut Mett Peter Traxler 《Helvetica chimica acta》1994,77(1):59-69
β-Nitrostyrene derivatives of adenosine 5′-glutarates are potent and selective bisubstrate-type inhibitors of the epidermal growth factor receptor protein tyrosine kinase (EGF-R PTK). In an attempt to improve the inhibitory activity, this type of compounds was modified with alkyl spacers of varying length between the nitrostyrene and the glutaryl units. The spacers consisted of 1, 3, 4, and 5 atoms to give compounds of the benzyl, oxyethyl, oxypropyl, and oxybutyl series, respectively (Schemes 1 and 2). Adenosine 5′-esters were prepared in the benzyl and oxypropyl series only. Compared to the compounds in the parent series without spacer (IC50 = 0.7–12 μM ), most of the modified compounds inhibited the EGF-R PTK only marginally or were inactive (IC50 ≥ 100 μM ). The only exceptions were the free acids 19 and 20 with IC50 values of ca. 5 μM . It is noteworthy that esterification of these two hydrogen glutarates with either MeOH or adenosine yielded inactive compounds, which is in contrast to the corresponding substances without spacers. 相似文献
10.
Xiaojun Zhou Riming Huang Jing Hao Huijuan Huang Manqin Fu Zhifang Xu Yongmei Zhou Xu‐E Li Samuel X. Qiu Bin Wang 《Helvetica chimica acta》2011,94(11):2092-2098
Two new prenylated xanthones (=9H‐xanthen‐9‐ones), garcimangosxanthones D ( 1 ) and E ( 2 ), together with the six known xanthones 3 – 8 , were isolated from the pericarp of Garcinia mangostana. Their structures were determined by analysis of their spectroscopic data. All of the isolated compounds were biologically evaluated for their in vitro cytotoxic activity against A549, Hep‐G2, and MCF‐7 human‐cancer cell lines and antioxidant activity. Compound 1 exhibited moderate cytotoxicity against Hep‐G2 (IC50=19.2 μM ) and weak cytotoxicity against MCF‐7 (IC50=62.8 μM ) cell lines, and compound 2 showed moderate cytotoxicity against A549, Hep‐G2, and MCF‐7 cell lines with IC50 values of 12.5–20.0 μM (Table 2). Both compounds 1 and 2 demonstrated a weak antioxidant activity with ferric reducing antioxidant power (FRAP) values of 41±7 and 130±4 μmol/g, respectively (Table 3). 相似文献
11.
KhalidMohammed Khan GhulamMurtaza Maharvi Ahmed Abbaskhan Safdar Hayat MahmudTareqHassan Khan Talat Makhmoor M.Iqbal Choudhary Farzana Shaheen Atta‐ur‐Rahman 《Helvetica chimica acta》2003,86(2):457-464
Phytochemical investigation on the whole plant of Salsola foetida resulted in the isolation of three new phenolic compounds 1, 2 , and 3 , which exhibit tyrosinase inhibition with moderate antioxidant activity. Compounds 1 – 3 inhibited tyrosinase with IC50 2.61, 1.85, and 0.40 μM , while exhibiting DPPH radical scavenging activity with IC50 383, 427 and 378 μM , respectively. The structures of 1, 2 , and 3 were determined by modern spectroscopic techniques. 相似文献
12.
Li‐Chai Chen I‐Li Chen Chih‐Chiang Huang Chang‐Hui Liao Jhy‐Yih Chen Tai‐Chi Wang 《中国化学会会志》2010,57(6):1331-1340
Some oxime‐containing 3,4‐dihydroquinolin‐2(1H)‐one derivatives were synthesized and evaluated for their antiplatelet and antiproliferative activities. These compounds were synthesized via alkylation of hydroxyl precursors followed by the reaction with NH2OH. The preliminary assays indicated that (Z)‐7‐[2‐(4‐fluorophenyl)‐2‐(hydroxyimino)ethoxy]‐3,4‐dihydroquinolin‐2(1H)‐one (13c) is the most active against U46619 induced platelet aggregation with an IC50 value of 3.51 μM. For the inhibition of AA‐induced aggregation, (E)‐6‐[2‐(hydroxyimino)propoxy]‐3,4‐dihydroquinolin‐2(1H)‐one (15 ) is the most potent with an IC50 value of 1.85 μM. These oxime‐containing 3,4‐dihydroquinolin‐2(1H)‐one derivatives were inactive against thrombin induced platelet aggregation with an IC50 value of greater than 26.78 μM. For the antiproliferative activity, most of these oxime‐containing 3,4‐dihydroquinolin‐2(1H)‐one derivatives were inactive while (Z)‐7‐[2‐(hydroxyimino)‐2‐(naphthalen‐2‐yl)ethoxy]‐3,4‐dihydroquinolin‐2(1H)‐one (13a) exhibited only marginal activities with GI50 value of 7.63, 7.34 and 6.36 μM against the growth of NPC‐TW01, NCI‐H661, and Jurkat respectively. 相似文献
13.
《Journal of heterocyclic chemistry》2018,55(4):803-813
Series of novel pyrazolo[3,4‐d]pyrimidines as potential telomerase inhibitors were synthesized. Results of the antitumor assay indicated that compounds 4b , 5a – b , 13b , c , and 14a , b exhibited the most potent activity (IC50 from 39 to 43 μM) against Ehrlich ascites carcinoma cells (EAC). Also, the newly synthesized compounds were examined for telomerase inhibition by the known a TRAP assay. The results showed that compound 13c has remarkable inhibition activity with IC50 value of 30 μM. On the other hand, computational studies were performed to the titled compounds to get insight in their degree of recognition with the conserved amino acids of the telomerase enzyme active site (code: 3DU6) as promising lead in the cancer cure era. 相似文献
14.
Waqas Jamil Sorath Solangi Muhammad Ali Khalid Muhammad Khan Muhammad Taha Muhammad Yar Khuhawar 《Arabian Journal of Chemistry》2019,12(8):2262-2269
2-Hydroxy salicylhydrazide isatin hydrazone (L) and its Mn (II), Co (II), Ni (II), Cu (II), and Zn (II), metal complexes were synthesized. 1H NMR, UV–Vis, IR spectroscopy and elemental (CHN/S) analysis techniques were applied for characterization. TG/DTA techniques revealed that all the synthetic compounds are thermally stable up to 300 °C. They were found non-electrolytes in nature. Furthermore, all these complexes were evaluated for antiglycation and DPPH radical scavenging activities. They showed varying degree of activity with IC50 values between 168.23 and 269.0 μM in antiglycation and 29.63–57.71 μM in DPPH radical scavenging activity. Mn (II), Co (II), Ni (II), Cu (II), and Zn (II), metal complexes showed good antiglycation as well as DPPH radical scavenging activity. The IC50 values for antiglycation activity are 168.23 ± 2.37, 234.27 ± 4.33, 257.1 ± 6.43, 267.7 ± 8.43, 269.0 ± 8.56 Ni for Co, Zn, Mn, Cu, and Ni complexes, respectively, while IC50 value were found to be 29.63 ± 2.76, 31.13 ± 1.41, 35.16 ± 2.45, 43.53 ± 3.12, 57.71 ± 2.61 μM for Cu, Zn, Mn, Co and Ni complexes, respectively, for DPPH radical scavenging activity. These synthesized metal complexes were found to be better active than standards Rutin (IC50 = 294.46 μM) for anti-glycation, and tert-butyl-4-hydroxyanisole (IC50 = 44.7 μM) for DPPH radical scavenging activity. 相似文献
15.
From the carbolithiation of 6‐morpholino fulvene ( 3a ) and different ortho‐lithiated heterocycles (furan, thiophene and N‐methylpyrrole), the corresponding lithium cyclopentadienide intermediate ( 4a – c ) was formed. These three lithiated intermediates underwent a transmetallation reaction with TiCl4 resulting in morpholino‐functionalised titanocenes 5a – c . When these titanocenes were tested against LLC‐PK cells, the IC50 values obtained were of 58, 63 and 115 μM for titanocenes 5a – c respectively. The most cytotoxic titanocene 5a with an IC50 value of 58 μM is found to be approximately 20 times less cytotoxic than cis‐platin, which showed an IC50 value of 3.3 μM, when tested on the LLC‐PK cell line, and 10 times less cytotoxic than its dimethylamino‐functionalised analogue (Titanocene C , IC50 = 5.5 μM). 相似文献
16.
Annika Honold Clara Lettl Franziska Schindele Boris Illarionov Rainer Haas Matthias Witschel Adelbert Bacher Markus Fischer 《Helvetica chimica acta》2019,102(3)
A library of over 103 thousand compounds was screened for inhibitors of the IspD domain (2‐C‐methyl‐d ‐erythritol 4‐phosphate cytidylyl transferase domain) of the bifunctional IspDF protein from Helicobacter pylori using a photometric assay. Around 300 compounds showed IC50 values below 100 μm , and three compounds had IC50 values below 1 μm . A few IspD inhibitors could also inhibit the IspF domain (2‐C‐Methyl‐d ‐erythritol‐2,4‐cyclopyrophosphate synthase) of the IspDF protein. The most potent IspD inhibitors were tested as growth inhibitors of H. pylori. Several compounds showed inhibition of bacterial growth with IC50 in the single‐digit μm range. The most potent growth inhibitor had an IC50 value of 3.4 μm . The most potent growth inhibitor without measurable effect on eukaryotic cell viability had an IC50 value of 7.2 μm . 相似文献
17.
《Journal of Saudi Chemical Society》2022,26(3):101468
A series of 28 novel naproxen derivatives (4a-f, 5a-f, 6a-d, 7a-f, and 8a-f) have been designed, synthesized, and characterized. The synthesized derivatives were assessed as dual inhibitors for 15-lipoxygenase (LOX) and α-glucosidase enzymes and checked for cytotoxicity and ADME studies. The inhibitory potential of naproxen derivatives for 15- LOX was checked through two different methods, the UV absorbance method and the Chemiluminescence method. The biological activities result revealed that through the UV absorbance method, compound 4f (IC50 21.31 ± 0.32 µM) was found potent among the series followed by compounds 4e (IC50 36.53 ± 0.51 µM) and 4d (IC50 49.62 ± 0.12 µM) against standard drug baicalein (IC50 22.46 ± 1.32 µM) and quercetin (IC50 2.34 ± 0.35 µM), while through chemiluminescence method tested compounds showed significant 15-LOX inhibition at the range of IC50 1.13 ± 0.62 µM ?123.47 ± 0.37 µM. Among these compounds, 4e (IC50 1.13 ± 0.62 µM), 5b (IC50 1.19 ± 0.43 µM), 8c (IC50 1.23 ± 0.35 µM) were found most potent inhibitors against quercetin (IC50 4.86 ± 0.14 µM), and baicalein (IC50 2.24 ± 0.13 µM). The chemiluminescence method was found more sensitive than the UV method to identify 15-LOX inhibitors. Interestingly all synthesized compounds showed significant α-glucosidase inhibitory activity (IC50 1.0 ± 1.13 µM ? 367.2 ± 1.23 µM) even better than the standard drug acarbose (IC50 375.82 ± 1.76 µM), while compound 6c (IC50 1.0 ± 1.13 µM) and 7c (IC50 1.1 ± 1.17 µM) were found most potent compounds among the series even many folds better than the standard drug. The cell viability results showed that all compounds were less toxic, maintained cellular viability at the range of 99.8 ± 1.3% to 63.7 ± 1.5%. ADME and molecular docking studies supported drug-likeness and binding interactions of compounds with the targeted enzymes. 相似文献
18.
19.
Chuan‐Wen Sun Hai‐Feng Wang Jun Zhu Ding‐Rong Yang Jiahua Xing Jia Jin 《Journal of heterocyclic chemistry》2013,50(6):1374-1380
A series of novel symmetrical trans‐bis‐Schiff bases ( 11a , 11b , 11c , 11d , 11e , 11f , 11g , 11h , 11i , 11j , 11k , 11l , 11m ) were designed and prepared as novel anticancer analogues, with the trans‐configuration confirmed by X‐ray diffraction. Preliminary inhibitory effects of these compounds on CML K562 cell growth were investigated, and the potential analogue 11e showed an excellent anti‐leukemia activity (IC50=6.35 μg/mL), which is higher than that of the clinical drug 5‐fluorouracil (IC50=8.48 μg/mL). Complete assignments had been achieved for the title compounds by spectroscopic techniques, and their structure–activity relationships have been studied. 相似文献
20.
Ting Zeng Yan-Ran Tang Bin Li Shumaila Tasneem Han-Wen Yuan Yan-Zhe Jia 《Natural product research》2020,34(17):2482-2489
AbstractTwenty-four compounds were isolated from the roots of Polygonatum cyrtonema Hua, including a new octopamine dimer, named trans-bis(N-feruloyl)octopamine (1). The structure was established on the basis of spectroscopic and chemical methods. All the extracts and compounds were evaluated for cytotoxic and antioxidant activities by using MTT and chemiluminescence assay. The extracts showed activity against MCF-7 and HepG-2 cell lines from IC50 0.30 to 1.01 mg mL?1. Compound 3 exhibited activity against HepG-2 cell lines with IC50 8.99?μM. Compound 7 exhibited activity against Hela cell lines with IC50 2.53?μM and BGC-823 cell lines with IC50 7.77?μM. Moreover, compound 7 showed antioxidant with IC50 12?µM compared to the positive control with IC50 77?µM. Compound 16 exhibited activity against HepG-2 cell lines with IC50 1.05?μM and MCF-7 cell lines with IC50 1.89?μM. These results indicated that this plant might be potential in natural medicine and healthy food. 相似文献