Synthesis and biological evaluation of [4-(2-phenylethenesulfonylmethyl)phenyl]-quinazolin-4-yl-amines as orally active anti-cancer agents.
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.
Sharma
Vedula M
VM
Discovery Chemistry, Dr. Reddy's Laboratories, Discovery Research, Miyapur, Hyderabad 500-049, India. sarmavm@drreddys.com
Adi Seshu
K V
KV
Chandra Sekhar
V
V
Madan
Sachin
S
Vishnu
B
B
Babu
P Aravind
PA
Vamsee Krishna
C
C
Sreenu
J
J
Ravi Krishna
V
V
Venkateswarlu
A
A
Rajagopal
Sriram
S
Ajaykumar
R
R
Kumar
T Sravan
TS
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
D000970:Antineoplastic Agents; D011799:Quinazolines