Unknown

Dataset Information

0

Apoptosis Inducing 1,3,4-Oxadiazole Conjugates of Capsaicin: Their In Vitro Antiproliferative and In Silico Studies.

ABSTRACT: A series of 1,3,4-oxadiazole tethered capsaicin derivatives was prepared by using one point modification at the vanillyl-hydroxyl group of capsaicin. All the prepared capsaicinoids were evaluated for their antiproliferative activity against NCI-60 human cancer cell lines at 10 μM. Among the compounds tested, compound 20a exhibited good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC50 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively, compared to the parent natural product capsaicin. Further on, it significantly inhibited the colony formation in NCI-H460 in a dose dependent manner and enhanced the ROS effect. It also caused cell arrest at the S phase and induced apoptosis via suppressing the Pro parp marker. Compound 20a exhibited an antimigratory property and suppressed the expression of the VEGF marker in a dose dependent manner. Furthermore, compound 20a also suppressed the effects of the p-Erk, p-p38, and P-CNA makers. In silico studies supported the interaction of this class of compounds with the VEGFR2 protein.

SUBMITTER: Naaz F 

PROVIDER: S-EPMC8591727 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Apoptosis Inducing 1,3,4-Oxadiazole Conjugates of Capsaicin: Their <i>In Vitro</i> Antiproliferative and <i>In Silico</i> Studies.

Naaz Fatima F   Ahmad Faiz F   Lone Bilal Ahmad BA   Khan Arif A   Sharma Kalicharan K   IntzarAli   ShaharYar M M   Pokharel Yuba Raj YR   Shafi Syed S  

ACS medicinal chemistry letters 20211021 11

A series of 1,3,4-oxadiazole tethered capsaicin derivatives was prepared by using one point modification at the vanillyl-hydroxyl group of capsaicin. All the prepared capsaicinoids were evaluated for their antiproliferative activity against NCI-60 human cancer cell lines at 10 μM. Among the compounds tested, compound <b>20a</b> exhibited good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC<sub>50</sub> 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively, compared to the parent  ...[more]

Similar Datasets

Unknown 1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and <i>in silico</i> studies.
| S-EPMC8725909 | biostudies-literature
Unknown Design, Synthesis, In Silico and In Vitro Studies for New Nitric Oxide-Releasing Indomethacin Derivatives with 1,3,4-oxadiazole-2-thiol Scaffold.
| S-EPMC8267937 | biostudies-literature
Unknown Design, synthesis and <i>in vitro</i> antiproliferative activity of new thiazolidinedione-1,3,4-oxadiazole hybrids as thymidylate synthase inhibitors.
| S-EPMC7241536 | biostudies-literature
Unknown In silico ADME predictions and in vitro antibacterial evaluation of 2-hydroxy benzothiazole-based 1,3,4-oxadiazole derivatives.
| S-EPMC7751938 | biostudies-literature
Unknown Chalcone/1,3,4-Oxadiazole/Benzimidazole hybrids as novel anti-proliferative agents inducing apoptosis and inhibiting EGFR & BRAFV<sup>600E</sup>.
| S-EPMC10504751 | biostudies-literature
Unknown 1,3,4-oxadiazole derivatives: synthesis, characterization, antimicrobial potential, and computational studies.
| S-EPMC4131560 | biostudies-literature
Unknown Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer.
| S-EPMC8245078 | biostudies-literature
Unknown Molecular Docking, Computational, and Antithrombotic Studies of Novel 1,3,4-Oxadiazole Derivatives.
| S-EPMC6274789 | biostudies-literature
Unknown In Vitro and In Silico Evaluation of New 1,3,4-Oxadiazole Derivatives of Pyrrolo[3,4-d]pyridazinone as Promising Cyclooxygenase Inhibitors.
| S-EPMC8431030 | biostudies-literature
Unknown α-Glucosidase and α-Amylase Inhibitory Potentials of Quinoline-1,3,4-oxadiazole Conjugates Bearing 1,2,3-Triazole with Antioxidant Activity, Kinetic Studies, and Computational Validation.
| S-EPMC9414972 | biostudies-literature