The disease of
cancer has been ranked second after
cardiovascular diseases and plant-derived molecules have played an important role for the treatment of
cancer. Nine cytotoxic plant-derived molecules such as
vinblastine,
vincristine,
navelbine,
etoposide,
teniposide,
taxol,
taxotere,
topotecan and
irinotecan have been approved as anticancer drugs. Recently,
epothilones are being emerging as future potential anti-
tumor agents. However, targeted
cancer therapy has now been rapidly expanding and small organic molecules are being exploited for this purpose. Amongst target specific small organic molecules,
quinazoline was found as one of the most successful chemical class in
cancer chemotherapy as three drugs namely
Gefitinib,
Erlotinib and
Canertinib belong to this series. Now,
quinazoline related chemical classes such as
quinolines and
naphthyridines are being exploited in
cancer chemotherapy and a number of molecules such as compounds
EKB-569 (52),
HKI-272 (78) and
SNS-595 (127a) are in different phases of clinical trials. This review presents the synthesis of
quinolines and
naphthyridines derivatives, screened for anticancer activity since year 2000. The synthesis of most potent derivatives in each prototype has been delineated. A brief structure activity relationship for each prototype has also been discussed. It has been observed that
aniline group at C-4, aminoacrylamide substituents at C-6, cyano group at C-3 and
alkoxy groups at C-7 in the
quinoline ring play an important role for optimal activity. While aminopyrrolidine functionality at C-7, 2'-thiazolyl at N-1 and carboxy group at C-3 in 1,8-naphthyridine ring are essential for eliciting the cytotoxicity. This review would help the medicinal chemist to design and synthesize molecules for targeted
cancer chemotherapy.