TY - JOUR
T1 - Synthesis, antiproliferative, and antioxidant activities of substituted n-[(1,3,4-oxadiazol-2-yl) methyl] benzamines
AU - Ahsan, Mohamed Jawed
AU - Bhandari, Lakshya
AU - Makkar, Shally
AU - Singh, Rajan
AU - Hassan, Mohd Zaheen
AU - Geesi, Mohammed H.
AU - Bakht, Mohamed Afroz
AU - Jadav, Surender Singh
AU - Balaraju, Tuniki
AU - Riadi, Yassine
AU - Rani, Sandhya
AU - Khalilullah, Habibullah
AU - Gorantla, Vasubabu
AU - Hussain, Afzal
N1 - Publisher Copyright:
©2020 Bentham Science Publishers.
PY - 2020
Y1 - 2020
N2 - Background: Oxadiazole emerged as an important class of heterocyclic compound with diverse biological activities like anticancer, antitubercular, anticonvulsant, anti-tubulin, antimicrobial, anti-inflammatory, antioxidant etc. Objective: The objective of this study is to synthesis series of twelve substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) and their evaluation as antiproliferative and antioxidant agents. Methods: The substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) analogues were synthesized as per the reported procedure. The antiproliferative activity was tested against nine different panels cancer cell lines (leukemia, colon, renal, non-small cell lung, breast, CNS, melanoma, prostate, and ovarian cancer) at 10 μM drug concentrations as per the NCI US Protocol. Results: 2-(5-((3-Chloro-4-fluorophenylamino)methyl)-1,3,4-oxadiazol-2-yl)phenol (6e) revealed the significant antiproliferative activity among the series of title compounds (6a-l). The compound, 6e showed maximum sensitivity towards CCRF-CEM, MCF-7, MOLT-4, T-47D, and SR cell lines with percent growth inhibitions (%GIs) of 79.92, 56.67, 39.62, 34.71 and 33.35, respectively. Furthermore, the compounds, 6e and 6c showed promising antioxidant activity with an IC50 value of 15.09 and 19.02 μM, respectively in DPPH free radicals (FR) scavenging activity. Conclusion: The present study may support a significant value in cancer drug discovery programme.
AB - Background: Oxadiazole emerged as an important class of heterocyclic compound with diverse biological activities like anticancer, antitubercular, anticonvulsant, anti-tubulin, antimicrobial, anti-inflammatory, antioxidant etc. Objective: The objective of this study is to synthesis series of twelve substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) and their evaluation as antiproliferative and antioxidant agents. Methods: The substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) analogues were synthesized as per the reported procedure. The antiproliferative activity was tested against nine different panels cancer cell lines (leukemia, colon, renal, non-small cell lung, breast, CNS, melanoma, prostate, and ovarian cancer) at 10 μM drug concentrations as per the NCI US Protocol. Results: 2-(5-((3-Chloro-4-fluorophenylamino)methyl)-1,3,4-oxadiazol-2-yl)phenol (6e) revealed the significant antiproliferative activity among the series of title compounds (6a-l). The compound, 6e showed maximum sensitivity towards CCRF-CEM, MCF-7, MOLT-4, T-47D, and SR cell lines with percent growth inhibitions (%GIs) of 79.92, 56.67, 39.62, 34.71 and 33.35, respectively. Furthermore, the compounds, 6e and 6c showed promising antioxidant activity with an IC50 value of 15.09 and 19.02 μM, respectively in DPPH free radicals (FR) scavenging activity. Conclusion: The present study may support a significant value in cancer drug discovery programme.
KW - Anti-proliferative agents
KW - Antioxidants
KW - DPPH
KW - Free radicals scavenging activity
KW - One dose assay
KW - Oxadiazoles
UR - http://www.scopus.com/inward/record.url?scp=85079887681&partnerID=8YFLogxK
U2 - 10.2174/1570180816666181113110033
DO - 10.2174/1570180816666181113110033
M3 - Article
AN - SCOPUS:85079887681
SN - 1570-1808
VL - 17
SP - 145
EP - 154
JO - Letters in Drug Design and Discovery
JF - Letters in Drug Design and Discovery
IS - 2
ER -
