- Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines
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A series of triphenyl substituted pyrimidines as analogous of colchicine and combretastatin A-4 was synthesized and evaluated for the antiproliferative potential. The compounds were screened against MDA-MB-231, HCT-116 and HT-29 cell lines using MTT assay. Most of the compounds displayed antiproliferative activity in low to sub micro molar concentration. Amongst the synthesized derivatives, compounds HK-2, HK-10 and HK-13 were found to be effective against all the three cancer cell lines. HK-2 exhibited IC50 values of 3.39 μM, 4.78 μM and 4.23 μM, HK-10 showed IC50 values of 0.81 μM, 5.89 μM, 4.96 μM and HK-13 showed IC50 values 3.24 μM, 4.93 μM and 4.73 μM against MDA-MB-231, HCT-116 and HT-29 cancer cell lines, respectively. HK-10 was found to be the most potent compound in the series with IC50 values of 0.81 μM against MDA-MB-231. In the cell cycle analysis, HK-2 and HK-10 showed cell arrest at G2/M phase of the cell cycle while HK-13 inhibited cell growth at the G1/G0 phase. All the three compounds showed cell death induced through apoptosis. In the docking studies, HK-2, HK-10 and HK-13 were found to fit well in the colchicine binding site of the tubulin. Some of the compounds in the current series were found to be promising against all the three cancer cell lines and may act as potent leads for further development.
- Ranjan Dwivedi, Ashish,Kumar, Vijay,Kaur, Harmeet,Kumar, Naveen,Prakash Yadav, Ravi,Poduri, Ramarao,Baranwal, Somesh,Kumar, Vinod
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supporting information
(2020/08/13)
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- Bi(OTf)3 catalyzed disproportionation reaction of cinnamyl alcohols
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Bi(OTf)3 catalyzed disproportionation reaction of cinnamyl alcohols provides chalcones and benzyl styrenes. The use of various metal triflates is investigated herein for facile and efficient redox transformation. A plausible mechanism has been proposed.
- Chan, Chieh-Kai,Tsai, Yu-Lin,Chang, Meng-Yang
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p. 3368 - 3376
(2017/05/22)
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- One-pot synthesis of cinnamylideneacetophenones and their in vitro cytotoxicity in breast cancer cells
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A series of cinnamylideneacetophenones were synthesized via a modified Claisen-Schmidt condensation reaction and evaluated for cytotoxicity against breast cancer cells using the Alamar Blue assay. Derivatives 17 and 18 bearing a 2-nitro group on the B rin
- Weldon, David J.,Saulsbury, Marilyn D.,Goh, Joshua,Rowland, Leah,Campbell, Petreena,Robinson, Laijia,Miller, Calvin,Christian, Joshua,Amis, Louisa,Taylor, Nia,Dill, Cassandra,Davis Jr., Willie,Evans, Stanley L.,Brantley, Eileen
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p. 3381 - 3384
(2014/07/22)
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- NUCLEAR RECEPTOR MODULATORS AND THEIR USE FOR THE TREATMENT AND PREVENTION OF CANCER
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Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.
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Page/Page column 25
(2013/02/28)
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- Carbonylative heck reactions using CO generated ex situ in a two-chamber System
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Chemical equations presented. A carbonylative Heck reaction of aryl iodides and styrene derivatives employing a two-chamber system using a stable, crystalline, and nontransition metal based carbon monoxide source is reported. By applying near-stoichiometr
- Hermange, Philippe,Gogsig, Thomas M.,Lindhardt, Anders T.,Taaning, Rolf H.,Skrydstrup, Troels
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supporting information; experimental part
p. 2444 - 2447
(2011/07/09)
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- Structure - Activity relationship studies of chalcone leading to 3-hydroxy-4,3′,4′,5′-tetramethoxychalcone and its analogues as potent nuclear factor κB inhibitors and their anticancer activities
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Chalcone is a privileged structure, demonstrating promising anti-inflammatory and anticancer activities. One potential mechanism is to suppress nuclear factor kappa B (NF-κB) activation. The structures of chalcone-based NF-κB inhibitors vary significantly that there is minimum information about their structure-activity relationships (SAR). This study aims to establish SAR of chalcone-based compounds to NF-κB inhibition, to explore the feasibility of developing simple chalcone-based potent NF-κB inhibitors, and to evaluate their anticancer activities. Three series of chalcones were synthesized in one to three steps with the key step being aldol condensation. These candidates demonstrated a wide range of NF-κB inhibitory activities, some of low micromolar potency, establishing that structural complexity is not required for NF-κB inhibition. Lead compounds also demonstrate potent cytotoxicity against lung cancer cells. Their cytotoxicities correlate moderately well with their NF-κB inhibitory activities, suggesting that suppressing NF-κB activation is likely responsible for at least some of the cytotoxicities. One lead compound effectively inhibits lung tumor growth with no signs of adverse side effects.
- Srinivasan, Balasubramanian,Johnson, Thomas E.,Lad, Rahul,Xing, Chengguo
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experimental part
p. 7228 - 7235
(2010/08/19)
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- Gallic acid-based indanone derivatives as anticancer agents
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Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds 10, 11, 12 and 14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (10, IC50 = 2.2 μM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100 μg/ml, 258 μM). While, indanones 11, 12 and 14 showed toxicities to erythrocytes at higher concentrations.
- Saxena, Hari Om,Faridi, Uzma,Srivastava, Suchita,Kumar,Darokar,Luqman, Suaib,Chanotiya,Krishna, Vinay,Negi, Arvind S.,Khanuja
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scheme or table
p. 3914 - 3918
(2009/04/07)
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