title: Synthesis and biological evaluation of [4-(2-phenylethenesulfonylmethyl)phenyl]-quinazolin-4-yl-amines as orally active anti-cancer agents.
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.
authors.affiliation: Discovery Chemistry, Dr. Reddy's Laboratories, Discovery Research, Miyapur, Hyderabad 500-049, India. sarmavm@drreddys.com
authors.forename: Vedula M
authors.initials: VM
authors.lastname: Sharma
authors.forename: K V
authors.initials: KV
authors.lastname: Adi Seshu
authors.forename: V
authors.initials: V
authors.lastname: Chandra Sekhar
authors.forename: Sachin
authors.initials: S
authors.lastname: Madan
authors.forename: B
authors.initials: B
authors.lastname: Vishnu
authors.forename: P Aravind
authors.initials: PA
authors.lastname: Babu
authors.forename: C
authors.initials: C
authors.lastname: Vamsee Krishna
authors.forename: J
authors.initials: J
authors.lastname: Sreenu
authors.forename: V
authors.initials: V
authors.lastname: Ravi Krishna
authors.forename: A
authors.initials: A
authors.lastname: Venkateswarlu
authors.forename: Sriram
authors.initials: S
authors.lastname: Rajagopal
authors.forename: R
authors.initials: R
authors.lastname: Ajaykumar
authors.forename: T Sravan
authors.initials: TS
authors.lastname: Kumar
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000138:chemical synthesis*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005260:Female; D019073:HT29 Cells; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D011799:Quinazolines / Q000008:administration & dosage* / Q000138:chemical synthesis*; D023041:Xenograft Model Antitumor Assays / Q000379:methods / Q000706:statistics & numerical data
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines