Title:Recent Developments in Oxazole Derivatives as Anticancer Agents: Review on
Synthetic Strategies, Mechanism of Action and SAR Studies
Volume: 22
Issue: 10
Author(s): Swanand Kulkarni, Kamalpreet Kaur and Vikas Jaitak*
Affiliation:
- Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghudda, Bathinda 151 401, India
Keywords:
Oxazole, anticancer, synthesis, mechanism of action, SAR, apoptosis.
Abstract:
Background: Cancer is the world’s third deadliest disease. Despite the availability of numerous treatments,
researchers are focusing on the development of new drugs with no resistance and toxicity issues. Many newly synthesized
drugs fail to reach clinical trials due to poor pharmacokinetic properties. Therefore, there is an imperative requisite
to expand novel anticancer agents with in vivo efficacy.
Objective: This review emphasizes synthetic methods, contemporary strategies used for the inclusion of oxazole moiety,
mechanistic targets, along with comprehensive structure-activity relationship studies to provide perspective into the
rational design of highly efficient oxazole-based anticancer drugs.
Methods: Literature related to oxazole derivatives engaged in cancer research is reviewed. This article gives a detailed
account of synthetic strategies, targets of oxazole in cancer, including STAT3, Microtubules, G-quadruplex, DNA
topoisomerases, DNA damage, protein kinases, miscellaneous targets, in vitro studies, and some SAR studies.
Results: Oxazole derivatives possess potent anticancer activity by inhibiting novel targets such as STAT3 and Gquadruplex.
Oxazoles also inhibit tubulin protein to induce apoptosis in cancer cells. Some other targets such as DNA
topoisomerase enzyme, protein kinases, and miscellaneous targets including Cdc25, mitochondrial enzymes, HDAC,
LSD1, HPV E2 TAD, NQO1, Aromatase, BCl-6, Estrogen receptor, GRP-78, and Keap-Nrf2 pathway are inhibited by
oxazole derivatives. Many derivatives showed excellent potencies on various cancer cell lines with IC50 values in nanomolar
concentrations.
Conclusion: Oxazole is a five-membered heterocycle, with oxygen and nitrogen at 1 and 3 positions, respectively. It is
often combined with other pharmacophores in the expansion of novel anticancer drugs. In summary, oxazole is a promising
entity to develop new anticancer drugs.