Synthesis and biological evaluation of [4-(2-phenylethenesulfonylmethyl)phenyl]-quinazolin-4-yl-amines as orally active anti-cancer agents |
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| Authors: | Sharma Vedula M Adi Seshu K V Chandra Sekhar V Madan Sachin Vishnu B Babu P Aravind Vamsee Krishna C Sreenu J Ravi Krishna V Venkateswarlu A Rajagopal Sriram Ajaykumar R Kumar T Sravan |
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| Institution: | Discovery Chemistry, Dr. Reddy's Laboratories, Discovery Research, Miyapur, Hyderabad 500-049, India. sarmavm@drreddys.com |
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| Abstract: | A new series of 4-(2-phenylethenesulfonylmethyl)phenyl]quinazolin-4-yl-amines was prepared and tested for its in vitro cytotoxic activity against a panel of 12 human cancer cell lines. Compounds 9, 15, 24 and 31 showed good in vitro activity and were further tested for their in vivo efficacy in the HT-29 human colon adeno carcinoma xenograft model. Compound 9 exhibited promising activity in this model. Dose-response studies for this compound against HT-29 human colon adeno carcinoma xenografts at 100, 200 and 400mg/kg doses were performed. |
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