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1.
Divakar Vishwanath Swamy S. Girimanchanaika Dukanya Dukanya Shobith Rangappa Ji-Rui Yang Vijay Pandey Peter E. Lobie Basappa Basappa 《Molecules (Basel, Switzerland)》2022,27(3)
Novel PARP inhibitors with selective mode-of-action have been approved for clinical use. Herein, oxadiazole based ligands that are predicted to target PARP-1 have been synthesized and screened for the loss of cell viability in mammary carcinoma cells, wherein seven compounds were observed to possess significant IC50 values in the range of 1.4 to 25 µM. Furthermore, compound 5u, inhibited the viability of MCF-7 cells with an IC50 value of 1.4µM, when compared to Olaparib (IC50 = 3.2 µM). Compound 5s also decreased cell viability in MCF-7 and MDA-MB-231 cells with IC50 values of 15.3 and 19.2 µM, respectively. Treatment of MCF-7 cells with compounds 5u and 5s produced PARP cleavage, H2AX phosphorylation and CASPASE-3 activation comparable to that observed with Olaparib. Compounds 5u and 5s also decreased foci-formation and 3D Matrigel growth of MCF-7 cells equivalent to or greater than that observed with Olaparib. Finally, in silico analysis demonstrated binding of compound 5s towardsthe catalytic site of PARP-1, indicating that these novel oxadiazoles synthesized herein may serve as exemplars for the development of new therapeutics in cancer. 相似文献
2.
C.?V.?Kavitha S.?Lakshmi Basappa K.?Mantelingu M.?A.?Sridhar J.?Shashidhara?Prasad K.?S.?RangappaEmail author 《Journal of chemical crystallography》2005,35(12):957-963
1-(cyano-(4-methoxyphenyl) methyl cyclohexanol(2), C24H32N2O2, a Venlafaxine intermediate is found to crystallize in both monoclinic(2a) and orthorhombic(2b) crystal systems. The form2a crystallizes in the space groupC2/c with the cell parametersa = 23.506(3),b = 5.550(3),c = 23.192(3), and β = 115.116(2)^∘.2b crystallizes in space groupP212121 with cell parametersa = 5.7850(6),b = 11.2680(6), andc = 20.6730(19). The intermolecular hydrogen bonding in the case of the monoclinic polymorph leads to the formation of dimer.
The synthesis, characterization, and crystal structure studies of Venlafaxine analog 1-[2-1-(4-dimethylamino-phenyl)-ethylideneamino]-1-(4-methoxy-phenyl)-ethyl]-cyclohexanol(4) is reported.4 crystallizes inP―1 space group with cell parametersa = 10.801(7),b = 12.078(7),c = 9.928(5), α = 96.12(5)^∘, β = 110.49(5)^∘, and γ = 112.42(6)^∘. 相似文献
3.
Several surfactant molecules self-assemble in solution to form long, cylindrical, flexible wormlike micelles. These micelles
can be entangled with each other leading to viscoelastic phases. The rheological properties of such phases are very interesting
and have been the subject of a large number of experimental and theoretical studies in recent years. We shall report our recent
work on the macrorheology, microrheology and nonlinear flow behaviour of dilute aqueous solutions of a surfactant CTAT (Cetyltrimethylammonium
Tosilate). This system forms elongated micelles and exhibits strong viscoelasticity at low concentrations (∼0.9 wt%) without
the addition of electrolytes. Microrheology measurements of G(θ) have been done using diffusing wave spectroscopy which will be compared with the conventional frequency sweep measurements
done using a cone and plate rheometer. The second part of the paper deals with the nonlinear rheology where the measured shear
stress σ is a nonmonotonic function of the shear rate
. In stress-controlled experiments, the shear stress shows a plateau for
larger than some critical strain rate, similar to the earlier reports on CPyCl/NaSal system. Cates et al have proposed that the plateau is a signature of mechanical instability in the form of shear bands. We have carried out extensive
experiments under controlled strain rate conditions, to study the time-dependence of shear stress. The measured time series
of shear stress has been analysed in terms of correlation integral and Lyapunov exponent to show unambiguously that the behaviour
is typical of low dimensional dynamical systems. 相似文献
4.
K.?Jayalakshmi M.?Mahendra Basappa B.H.?Doreswamy M.A.?Sridhar J.?Shashidhara?Prasad K.S.?RangappaEmail author 《Journal of chemical crystallography》2005,35(1):67-70
The title compound (C22H19NOS) was synthesized, characterized and structure was determined by X-ray diffraction method. It crystallizes in the monoclinic space group P21/c with cell parameters a = 22.181(2) Å, b = 6.0760(4) Å, c = 13.349(3) Å, = 95.615(3)^, and {Z = 4}. The final residual factor is 0.0625 for 1724 reflections with I > 2(I). 4-thiazolidinone ring moiety shows twisted conformation. 相似文献
5.
G. Basappa N.V. Madhusudana 《The European Physical Journal B - Condensed Matter and Complex Systems》1998,1(2):179-187
We present experimental studies on the effect of strong electric fields on the nematogen p-cyanophenyl p-n-heptyl benzoate
which has the strongly polar cyano end group and a large positive dielectric anisotropy. We use a local temperature measurement
to take into account heating effects and an electrical impedance analysis to determine both the dielectric constant () and the resistance (R) of the sample. We also measure the higher harmonic responses of the medium. The new results obtained in this study are: (i)
a detailed temperature dependence of the terms which describe (a) the quenching of macroscopic thermal fluctuations of the
nematic director and (b) the enhancement of the orientational order parameter due to Kerr effect, (ii) clear evidence for
the critical divergence of susceptibility as reflected in the third harmonic signal, (iii) an unusual enhancement of the conductivity
which shows a large peak just below the critical point , (iv) a significant peak in the second harmonic signal at and (v) evidence for a field induced nematic-nematic transition well inside the nematic range. We argue that the results
(iii)-(v) indicate the presence of polar short range order in the medium and hence support a molecular model in which such an order has been proposed.
Received: 15 July 1997 / Received in final form: 24 September 1997 / Accepted: 29 October 1997 相似文献
6.
7.
Nivedita Rathnakar Desai Krishnaswamy Gurunathan Parameshwar Adimule Suchetan Aruna Kumar Doyjide Basappa Shivalingegowda Naveen Neratur Krishnappagowda Lokanath Swamy Sreenivasa 《Research on Chemical Intermediates》2017,43(11):6131-6154
The present work reports the synthesis of novel 2-(4-(4-substitutedphenylsulfonyl) piperazin-1-yl) quinolone-3-carbaldehyde derivatives, namely, 2-(4-tosylpiperazin-1-yl)quinoline-3-carbaldehyde (4a), 2-(4-(4-nitrophenylsulfonyl)piperazin-1-yl)quinoline-3-carbaldehyde (4b) and 2-(4-(4-tert-butylphenylsulfonyl) piperazin-1-yl)quinoline-3-carbaldehyde (4c). These compounds have been characterized by FT-IR, 1H-NMR, 13C-NMR and LCMS. Further, the structures of compounds 4b and 4c have been elucidated by single crystal X-ray diffraction studies. The asymmetric unit of 4b contains two molecules (A and B) and that of 4c contains one. The piperazine ring in both the molecules 4b and 4c has chair conformation and the aldehyde group is twisted with respect to the quinoline group, respectively, by 13.3 (3)°, 18.2 (3)° and 11.2 (3)° in Molecule A & B of 4b and 4c due to the bulky piperazinyl group present in the ortho position. The crystal structures of both features interactions of the type C-H…O, C-H…πaryl and πaryl… πaryl, leading to a three-dimensional (3D) supramolecular architecture in 4b and a one-dimensional (1D) architecture in 4c. The various intermolecular interactions exhibited in 4b and 4c are well supported by Hirshfeld surface and fingerprint plots analysis. Further, the three compounds were evaluated for their in-silico antimicrobial activity. In-silico molecular docking studies were carried out in order to know the binding modes of the synthesized compounds with DNA Gyrase A and N-myristoyltranferase as target proteins for antibacterial and antifungal docking studies, respectively. 相似文献
8.
Sadashiva Maralinganadoddi Panchegowda Basappa NanjundaSwamy Shivananju Li Feng Manu Kanjoormana Aryan Sengottuvelan Murugan Prasanna Doddakunche Shivaramu Anilkumar Nirvanappa Chikkagundagal Sethi Gautam Sugahara Kazuyuki Rangappa Kanchugarakoppal Subbegowda 《BMC chemical biology》2012,12(1):1-11
Background
Nef is an HIV-1 accessory protein essential for viral replication and AIDS progression. Nef interacts with a multitude of host cell signaling partners, including members of the Src kinase family. Nef preferentially activates Hck, a Src-family kinase (SFK) strongly expressed in macrophages and other HIV target cells, by binding to its regulatory SH3 domain. Recently, we identified a series of kinase inhibitors that preferentially inhibit Hck in the presence of Nef. These compounds also block Nef-dependent HIV replication, validating the Nef-SFK signaling pathway as an antiretroviral drug target. Our findings also suggested that by binding to the Hck SH3 domain, Nef indirectly affects the conformation of the kinase active site to favor inhibitor association. 相似文献9.
K. R. Ravi Kumar Basappa K. S. Rangappa H. Mallesha 《Journal of heterocyclic chemistry》2003,40(4):607-609
A selective reduction and its subsequent cyclisation of novel isoxazolidines into γ‐lactams have been examined in presence of Raney ‐ nickel catalyst. 相似文献
10.
Synthesis,Characterization, Novel Interaction of DNA,Antioxidant and Antimicrobial Studies of New Water Soluble Metallophthalocyanines Posture Eight Hydroxyphenyl Moiety via 1,3,4‐oxadiazole Bridge
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Chidananda Basappa Venugopala K. R. Reddy Harish M. N. Kotresh Pradeep K. Musturappa Mruthyunjayachari C. Devendrachari Shimoga D. Ganesh 《Journal of heterocyclic chemistry》2015,52(6):1782-1791
The new peripheral 2(3),9(10),16(17),23(24)‐tetra‐5‐[4,4′‐diphenol]‐phenyl‐[1,3,4]‐oxadiazole substituted metallophthalocyanine (MPc) complexes has been well designed and executed. Due to high conjugation and excellent solubility in water makes them potential use in DNA binding and cleavage studies. Fourier transform infrared spectroscopy, nuclear magnetic resonance, electron spin ionization mass spectra data, and elemental analysis confirmed the well‐defined saddle‐like distorted structures for these substituted MPc complexes. The successful synthesis of these novel water soluble MPc moieties were employed as an effective DNA binding with calf thymus DNA was monitored using ultraviolet?visible spectral titrations and cleavage pBR322 DNA conceded in the absence of reductant by agarose gel electrophoresis method. The results indicate that all these water soluble complexes significantly show excellent binding and modest cleavage sensitivity activity. It is noteworthy that 6 and 7 exhibit potential antimicrobial and appreciable antioxidant activity with other water soluble phthalocyanines. 相似文献