- Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents
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A new series of 1,3-biarylsulfanyl derivatives (homodibenzyl core motif) have been designed and synthesized as new estrogen receptor ligands by chopping benzothiophene core of raloxifene to engender seco-raloxifene scaffold. All the synthesized compounds were screened for anti-proliferative, anti-osteoporotic, and anti-implantation activity. Compounds (35, 36) having basic amino anti-estrogenic side chain were exhibiting potential anti-proliferative activity in MCF-7, MDA-MB-231 and ishikawa cell lines. Some of the synthesized compounds having homodibenzyl motif (5, 8, 10) have shown moderate anti-osteoporotic activity.
- Kumar, Atul,Tripathi, Vishwa Deepak,Kumar, Promod,Gupta, Lalit Prakash,Akanksha,Trivedi, Ritu,Bid, Hemant,Nayak,Siddiqui, Jawed A.,Chakravarti, Bandana,Saxena, Ruchi,Dwivedi, Anila,Siddiquee,Siddiqui,Konwar, Rituraj,Chattopadhyay, Naibedya
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scheme or table
p. 5409 - 5419
(2011/10/31)
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- 1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: A novel series of thrombin inhibitors
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A novel series of 1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing an amine moiety was identified as thrombin inhibitors. An indole with basic diamine moieties (12a) was the most potent thrombin inhibitor in the series with K(ass) = 197 x 106 L/mol. (C) 2000 Elsevier Science Ltd.
- Takeuchi, Kumiko,Bastian, Jolie A.,Gifford-Moore, Donetta S.,Harper, Richard W.,Miller, Shawn C.,Mullaney, Jeffrey T.,Sall, Daniel J.,Smith, Gerald F.,Zhang, Minsheng,Fisher, Matthew J.
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p. 2347 - 2351
(2007/10/03)
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- Chemotherapeutic nitroheterocycles. 18. 2 (5 Nitro 2 imidazolylmethylene) 1 indanones, 1 tetralones, and acetophenones substituted by aminoalkoxy groups
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2 (5 Nitro 2 imidazolylmethylene) 1 indanones; 1 tetralones, and acetophenones with aminoalkoxy substituents, groups and related compounds, were synthesized and their antimicrobial activities were evaluated. Some of these compounds surprisingly exhibited a broad antibacterial spectrum including Proteus species and Pseudomonas aeruginosa. High antitrichomonal activities were also observed in vitro minimum inhibitory concentration of 0.0004 μg/ml) and six compounds displayed in vivo activity against Trichomonas vaginalis in mice comparable to that of metronidazole.
- Rufer,Kessler,Schroeder
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p. 253 - 258
(2007/10/05)
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