- A novel series of benzothiazepine derivatives as tubulin polymerization inhibitors with anti-tumor potency
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In this work, a series of diaryl benzo[b][1,4]thiazepine derivatives D1-D36 were synthesized and screened as tubulin polymerization inhibitors with anti-tumor potency. They were designed by introducing the seven-member ring benzothiazepine as the linker f
- Wang, Bin,Wang, Li-Ren,Liu, Lu-Lu,Wang, Wei,Man, Ruo-Jun,Zheng, Da-Jun,Deng, Yu-Shan,Yang, Yu-Shun,Xu, Chen,Zhu, Hai-Liang
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- Divergent Synthesis and Evaluation of the in vitro Cytotoxicity Profiles of 3,4-Ethylenedioxythiophenyl-2-propen-1-one Analogues
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A new series of 3,4-ethylenedioxythiophene (EDOT)-appended propenones were prepared by condensation reaction and their in vitro cytotoxicity effects were evaluated against five human cancer cell lines. Preliminary structure–activity relationships of EDOT-
- Karunakaran, Jayachandran,Dhatchana Moorthy, Nachiappan,Chowdhury, Somenath Roy,Iqbal, Saleem,Majumder, Hemanta K.,Gunasekaran, Krishnasamy,Vellaichamy, Elangovan,Mohanakrishnan, Arasambattu K.
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p. 1418 - 1430
(2019/08/07)
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- Synthetic compounds from an in house library as inhibitors of falcipain-2 from Plasmodium falciparum
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Falcipain-2 (FP-2) is a key cysteine protease from the malaria parasite Plasmodium falciparum. Many previous studies have identified FP-2 inhibitors; however, none has yet met the criteria for an antimalarial drug candidate. In this work, we assayed an in-house library of non-peptidic organic compounds, including (E)-chalcones, (E)-N'-benzylidene-benzohydrazides and alkyl-esters of gallic acid, and assessed the activity toward FP-2 and their mechanisms of inhibition. The (E)-chalcones 48, 54 and 66 showed the lowest IC50 values (8.5±0.8μM, 9.5±0.2μM and 4.9±1.3μM, respectively). The best inhibitor (compound 66) demonstrated non-competitive inhibition, and using mass spectrometry and fluorescence spectroscopy assays, we suggest a potential allosteric site for the interaction of this compound, located between the catalytic site and the hemoglobin binding arm in FP-2. We combined structural biology tools and mass spectrometry to characterize the inhibition mechanisms of novel compounds targeting FP-2.
- Bertoldo, Jean Borges,Chiaradia-Delatorre, Louise Domeneghini,Mascarello, Alessandra,Leal, Paulo César,Cordeiro, Marlon Norberto Sechini,Nunes, Ricardo José,Sarduy, Emir Salas,Rosenthal, Philip Jon,Terenzi, Hernán
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p. 299 - 307
(2015/04/14)
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- Chalcones: A new class of antimitotic agents
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A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-propen- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa
- Edwards,Stemerick,Sunkara
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p. 1948 - 1954
(2007/10/02)
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