TY - JOUR
T1 - 1,3,4-Oxadiazole-containing hybrids as potential anticancer agents
T2 - Recent developments, mechanism of action and structure-activity relationships
AU - Nayak, Swarnagowri
AU - Gaonkar, Santosh L.
AU - Musad, Ebraheem Abdu
AU - Dawsar, Abdullah Mohammed AL
N1 - Publisher Copyright:
© 2021 The Authors
PY - 2021/8
Y1 - 2021/8
N2 - Chemotherapy is an important therapeutic approach for the treatment of cancer. Currently, many anticancer drugs are available in the market that plays an important role in cancer treatment, but concerns such as, drug resistance and side effects create an urgent need for the development of new anti-tumor drugs with high potency and less side effects. Heterocycles are of great interest due to their fascinating anticancer activity. Among them, 1,3,4-oxadiazoles showed attracting anti-tumor activity and its derivatives are under clinical trials for the treatment of cancer. Hybridization of 1,3,4-oxadiazole moiety with other heterocyclic pharmacophoresis a promising approach to overcome various disadvantages of current anticancer drugs such as drug resistance, toxicity, and other side effects. Thus, 1,3,4-oxadiazole-heterocycle hybrids occupy a significant position in the discovery of anti-tumor drugs. Among the reported oxadiazole-based hybrids reviewed here, compounds 45i, 59j, and 62x showed the highest anticancer activity with IC50 values in the nanomolar range. This review summarizes the recent developments in the anticancer potential, structure–activity relationships, and mechanisms of actions of 1,3,4-oxadiazole-heterocycle hybrids.
AB - Chemotherapy is an important therapeutic approach for the treatment of cancer. Currently, many anticancer drugs are available in the market that plays an important role in cancer treatment, but concerns such as, drug resistance and side effects create an urgent need for the development of new anti-tumor drugs with high potency and less side effects. Heterocycles are of great interest due to their fascinating anticancer activity. Among them, 1,3,4-oxadiazoles showed attracting anti-tumor activity and its derivatives are under clinical trials for the treatment of cancer. Hybridization of 1,3,4-oxadiazole moiety with other heterocyclic pharmacophoresis a promising approach to overcome various disadvantages of current anticancer drugs such as drug resistance, toxicity, and other side effects. Thus, 1,3,4-oxadiazole-heterocycle hybrids occupy a significant position in the discovery of anti-tumor drugs. Among the reported oxadiazole-based hybrids reviewed here, compounds 45i, 59j, and 62x showed the highest anticancer activity with IC50 values in the nanomolar range. This review summarizes the recent developments in the anticancer potential, structure–activity relationships, and mechanisms of actions of 1,3,4-oxadiazole-heterocycle hybrids.
KW - 1,3,4-Oxadiazoles
KW - Anticancer activity
KW - Hybrid molecules
KW - Mechanisms of action
KW - Structure–activity relationships
UR - http://www.scopus.com/inward/record.url?scp=85108881251&partnerID=8YFLogxK
U2 - 10.1016/j.jscs.2021.101284
DO - 10.1016/j.jscs.2021.101284
M3 - Review article
AN - SCOPUS:85108881251
SN - 1319-6103
VL - 25
JO - Journal of Saudi Chemical Society
JF - Journal of Saudi Chemical Society
IS - 8
M1 - 101284
ER -
