Bibliographic Details
| Title: |
Design and synthesis of novel ureido and thioureido conjugated hydrazone derivatives with potent anticancer activity. |
| Authors: |
Koopaei, Nasrin Nassiri, Shademani, Mehrasa, Yazdi, Nasrin Shirzad, Tahmasvand, Raheleh, Dehbid, Mina, Koopaei, Mansur Nassiri, Azizian, Homa, Mousavi, Zahra, Almasirad, Ali, Salimi, Mona |
| Source: |
BMC Chemistry; 11/1/2022, Vol. 16 Issue 1, p1-15, 15p |
| Subject Terms: |
HYDRAZONE derivatives, ANTINEOPLASTIC agents, T helper cells, WESTERN immunoblotting, HEPATOCELLULAR carcinoma, STAINS & staining (Microscopy) |
| Abstract: |
Background: Compounds possessing urea/thiourea moiety have a wide range of biological properties including anticancer activity. On the other hand, taking advantage of the low toxicity and structural diversity of hydrazone derivatives, they are presently being considered for designing chemical compounds with hydrazone moiety in the field of cancer treatment. With this in mind, a series of novel ureido/thioureido derivatives possessing a hydrazone moiety bearing nitro and chloro substituents (4a–4i) have been designed, synthesized, characterized and evaluated for their in vitro cytotoxic effect on HT-29 human colon carcinoma and HepG2 hepatocarcinoma cell lines. Results: Two compounds (4c and 4e) having the chloro phenylurea group hybridized with phenyl hydrazone bearing nitro or chloro moieties demonstrated potent anticancer effect with the IC50 values between 2.2 and 4.8 µM at 72 h. The mechanism of action of compound 4c was revealed in hepatocellular carcinoma cells as an inducer of apoptosis in a caspase-independent pathway. Conclusion: Taken together, the current work presented compound 4c as a potential lead compound in developing future hepatocellular carcinoma chemotherapy drugs. Methods: The compounds were synthesized and then characterized by physical and spectral data (FT-IR, 1H-NMR, 13C-NMR, Mass). The anticancer activity was assessed using MTT assay, flowcytometry, annexin-V, DAPI staining and Western blot analysis. [ABSTRACT FROM AUTHOR] |
|
Copyright of BMC Chemistry is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) |
| Database: |
Complementary Index |
|
Full text is not displayed to guests. |
Login for full access.
|
