Novel anti-cancer drug COTI-2 synergizes with therapeutic agents and does not induce resistance or exhibit cross-resistance in human cancer cell lines

Background: In this study, two novel hybrid series of artemisinin and quinazolinones were synthesized and evaluated in vitro cytotoxicity against two human cancer cell lines, including SKLu-1 (lung cancer), MCF- 7 (breast cancer). The bio-assay results indicated that most of the target compounds exhibited cytotoxic activities against both human cancer cell lines tested, and seemed to be more cytotoxic toward the breast (MCF-7) cancer cells than lung (SKLu-1) cancer cells. Among the synthesized artemisinin hybrids, the compound 13d containing a quinazolinone conjugated system exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Objective: This study aims at developing novel hybrids of artemisinin and quinazolinones as anti-cancer agents. Method: A series of novel hybrids were designed, synthesized and evaluated for cytotoxicity against two human cancer cell lines, including SKLu-1 and MCF-7 using SRB method. Results : All thirteen hybrids of artemisinin with quinazolinone exhibited cytotoxic activity against two tested cancer cell lines, in which the compound 13d exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as leads for future design of hybrids and have the potential for further studies in the field of anti-cancer agent development.

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Phosphonium Salt Displays Cytotoxic Effects Against Human Cancer Cell Lines

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/187152061805180821121547 ◽

2018 ◽

Vol 18 (5) ◽

pp. 765-765

Author(s):

Dhanyalayam D ◽

Palma G ◽

Cappello AR ◽

Mariconda A ◽

Sinicropi MS ◽

...

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Medicinal Chemistry ◽

Phosphonium Salt ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Cytotoxic Effects ◽

Human Cancer Cell Lines ◽

Anti Cancer

Due to an oversight one of the author’s name was published wrong in the article entitled “Phosphonium Salt Displays Cytotoxic Effects Against Human Cancer Cell Lines” in “Anti-Cancer Agents in Medicinal Chemistry, 2015, Vol. 17, No. 13. pp. 1796.” <p> The correct names of all authors are given below: <p> Dhanyalayam D, Palma G, Cappello AR, Mariconda A, Sinicropi MS, Giordano F, Del Vecchio V, Ramunno A, Arra C, Longo P, Saturnino C.

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Synthesis and anti-cancer activities of glycosides and glycoconjugates of diterpenoid isosteviol

MedChemComm ◽

10.1039/c9md00242a ◽

2019 ◽

Vol 10 (8) ◽

pp. 1488-1498 ◽

Cited By ~ 2

Author(s):

Radmila R. Sharipova ◽

Mayya G. Belenok ◽

Bulat F. Garifullin ◽

Anastasiya S. Sapunova ◽

Alexandra D. Voloshina ◽

...

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Human Cancer Cell Lines ◽

Anti Cancer ◽

Mcf 7

A series of glycosides and glycoconjugates of diterpenoid isosteviol with various monosaccharide residues were synthesized. Most of them showed moderate to significant cytotoxicity against human cancer cell lines M-HeLa and MCF-7.

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