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Cancer continues to be a major health concern and a number of deaths are caused by cancer that is second only to cardiovascular
diseases. The development of compounds that target genes involved in cancer pathogenesis is a potential area of cancer drug
discovery. A number of anticancer drugs employed clinically exert their effect by inhibiting nucleic acid (DNA or RNA) or protein
synthesis. It is evident that DNA is an important cellular target for many anticancer agents. Pyrrolo[2,1-c][1,4]benzodiazepines
(PBDs) are naturally occurring compounds isolated from various Streptomyces species. The PBDs exert their biological activity
through covalent binding within the minor groove of DNA. Several PBD conjugates have been synthesized to investigate the
detailed biological aspects relating to the mechanism of action. Some of the potent molecules like PBD-quinazolinones and
PBD-diaryloxadiazoles have been evaluated for their in vivo efficacy studies. These studies suggest that such PBD conjugates
have promising anticancer activity. Some of the PBD conjugates act as activators of p53 and suppressors of NF-κB and thereby
they could be considered as promising anticancer agents with improved potential for the suppression of tumours. To improve the
selectivity as well as stability, some new β-galactoside prodrugs of PBDs have been synthesized and evaluated for their potential
use in selective therapy of solid tumors by ADEPT and PMT protocols. Another important property of these molecules is their
enhanced water solubility and stability, which are essential for a molecule to be an effective drug.
Ahmed Kamal graduated from Osmania University, Hyderabad (India) and did his Ph.D. research in the area of Medicinal Chemistry. He later joined
as a Scientist at the Indian Institute of Chemical Technology (IICT), Hyderabad. For the last 25 years, he has pursued his research career at IICT,
Hyderabad and is presently working as an Outstanding Scientist. He also holds an additional charge of Project Director of NIPER, Hyderabad. He
has over 290 publications, 12 review papers and 7 book chapters and has filed over 75 patents. He is serving as an editorial advisory board member
for the journals of repute.
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