Design and synthesis of a peptide derivative of ametantrone targeting the major groove of the d(GGCGCC)2 palindromic sequence

2020 ◽  
Vol 44 (9) ◽  
pp. 3624-3631
Author(s):  
Alberto Ongaro ◽  
Giovanni Ribaudo ◽  
Emmanuelle Braud ◽  
Mélanie Ethève-Quelquejeu ◽  
Michele De Franco ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Palindromic Sequence ◽  
Major Groove ◽  
Design And Synthesis ◽  
Peptide Derivative ◽  
Line P ◽  
Palindromic Sequences

We report the synthesis of a peptide derivative of antitumor anthraquinones, designed to target GC-rich palindromic sequences. It has micromolar activities on three cancer cell lines and is fifty times less toxic than mitoxantrone on a healthy line.

scholarly journals Design and synthesis of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone conjugates: study on their apoptosis inducing ability and tubulin polymerization inhibition

2020 ◽  
Vol 11 (11) ◽  
pp. 1295-1302
Author(s):  
Kesari Lakshmi Manasa ◽  
Sowjanya Thatikonda ◽  
Dilep Kumar Sigalapalli ◽  
Sowmya Vuppaladadium ◽  
Ganthala Parimala Devi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Proliferative Potential ◽  
Tubulin Polymerization ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Substituted 1

Herein, we have designed and synthesized a library of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone derivatives (10aa–ef) and evaluated for their anti-proliferative potential against a panel of human cancer cell lines.

ChemInform Abstract: Design and Synthesis of C35-Fluorinated Solamins and Their Growth Inhibitory Activities Against Human Cancer Cell Lines.

ChemInform ◽  
2012 ◽  
Vol 43 (9) ◽  
pp. no-no
Author(s):  
Naoto Kojima ◽  
Yuki Suga ◽  
Hiromi Hayashi ◽  
Takao Yamori ◽  
Takehiko Yoshimitsu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Growth Inhibitory ◽  
Inhibitory Activities

scholarly journals Design and Synthesis of Flavonoidal Ethers and Their Anti-Cancer Activity In Vitro

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1749 ◽  
Author(s):  
Lu Jin ◽  
Meng-Ling Wang ◽  
Yao Lv ◽  
Xue-Yi Zeng ◽  
Chao Chen ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Cancer Drug ◽  
Hydroxyl Groups ◽  
Drug Candidates ◽  
Design And Synthesis ◽  
Anti Cancer ◽  
Clinical Drugs

Flavonoids are well-characterized polyphenolic compounds with pharmacological and therapeutic activities. However, most flavonoids have not been developed into clinical drugs, due to poor bioavailability. Herein, we report a strategy to increase the drugability of flavonoids by constructing C(sp2)-O bonds and stereo- as well as regioselective alkenylation of hydroxyl groups of flavonoids with ethyl-2,3-butadienoate allenes. Twenty-three modified flavonoid derivatives were designed, synthesized, and evaluated for their anti-cancer activities. The results showed that compounds 4b, 4c, 4e, 5e, and 6b exhibited better in vitro inhibitory activity against several cancer cell lines than their precursors. Preliminary structure–activity relationship studies indicated that, in most of the cancer cell lines evaluated, the substitution on position 7 was essential for increasing cytotoxicity. The results of this study might facilitate the preparation or late-stage modification of complex flavonoids as anti-cancer drug candidates.

Rational design and synthesis of novel 2-(substituted-2H-chromen-3-yl)-5-aryl-1H-imidazole derivatives as an anti-angiogenesis and anti-cancer agent

RSC Advances ◽  
2014 ◽  
Vol 4 (99) ◽  
pp. 56489-56501 ◽  
Author(s):  
Gopinath Gudipudi ◽  
Someswar R. Sagurthi ◽  
Shyam Perugu ◽  
G. Achaiah ◽  
G. L. David Krupadanam
Keyword(s):  
Biological Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Rational Design ◽  
Cancer Cell Lines ◽  
Imidazole Derivatives ◽  
Design And Synthesis ◽  
Anti Cancer ◽  
Cancer Agent

Based on the earlier proven pharmacophore analogues of cancer a novel 2-(substituted-2H-chromen-3-yl)-5-aryl-1H-imidazoles were rationally designed, synthesized and used for competitive biological activity against cancer cell lines.

scholarly journals Design and synthesis of DNA-intercalative naphthalimide-benzothiazole/cinnamide derivatives: cytotoxicity evaluation and topoisomerase-IIα inhibition

MedChemComm ◽  
2019 ◽  
Vol 10 (1) ◽  
pp. 72-79 ◽  
Author(s):  
N. Sankara Rao ◽  
Narayana Nagesh ◽  
V. Lakshma Nayak ◽  
Satish Sunkari ◽  
Ramya Tokala ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Topoisomerase Iiα ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis

A new series of different naphthalimide-benzothiazole/cinnamide derivatives were designed, synthesized and tested for their in vitro cytotoxicity on selected human cancer cell lines.

Anticarcinogenic and metal chelation properties of novel hydroxybenzylidene-1-indanone derivatives in the U-251 glioblastoma cell line

2018 ◽  
Vol 42 (5) ◽  
pp. 3878-3884 ◽  
Author(s):  
Mariana Lozano-Gonzalez ◽  
María Teresa Ramírez-Apan ◽  
Antonio Nieto-Camacho ◽  
Ruben Alfredo Toscano ◽  
Ana Laura Sanchez-Sandoval ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Cytotoxic Agents ◽  
Glioblastoma Cell Line ◽  
Glioblastoma Cell ◽  
Metal Chelation ◽  
Line P

A novel series of (Z)-2-(hydroxy(aryl)methylene)-2,3-dihydro-1H-indanone derivatives were designed, synthesized and evaluated as cytotoxic agents against six cancer cell lines.

Sign in / Sign up

Export Citation Format

Share Document