Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole Derivatives against Pancreatic Cancer Cells*

Giovanna Li Petri, Stella Cascioferro, Btissame el Hassouni, Daniela Carbone, Barbara Parrino, Girolamo Cirrincione, Godefridus J. Peters, Patrizia Diana, Elisa Giovannetti

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds (1a-g) were submitted to National Cancer Institute (NCI). Remarkably, compound 1g showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory concentration of between 1.67 and 10.3 μM. Further studies showed antiproliferative activity of 1a-g and of three additional compounds 1h, 1i and 1l, with different substituents on the indole nucleus and phenyl ring, against three pancreatic cancer cell lines. In particular, derivatives 1g and 1h inhibited both proliferation and migration of SUIT-2 cells at concentrations lower than 10 μM. In conclusion, new indole derivatives are characterized by in vitro antitumor activity, supporting future mechanistic studies.
Original languageEnglish
Pages (from-to)3615-3620
JournalAnticancer Research
Volume39
Issue number7
DOIs
Publication statusPublished - 1 Jan 2019

Cite this

@article{7406b72f5dc644f38d989d5cf83e1d41,
title = "Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole Derivatives against Pancreatic Cancer Cells*",
abstract = "Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds (1a-g) were submitted to National Cancer Institute (NCI). Remarkably, compound 1g showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory concentration of between 1.67 and 10.3 μM. Further studies showed antiproliferative activity of 1a-g and of three additional compounds 1h, 1i and 1l, with different substituents on the indole nucleus and phenyl ring, against three pancreatic cancer cell lines. In particular, derivatives 1g and 1h inhibited both proliferation and migration of SUIT-2 cells at concentrations lower than 10 μM. In conclusion, new indole derivatives are characterized by in vitro antitumor activity, supporting future mechanistic studies.",
author = "{Li Petri}, Giovanna and Stella Cascioferro and {el Hassouni}, Btissame and Daniela Carbone and Barbara Parrino and Girolamo Cirrincione and Peters, {Godefridus J.} and Patrizia Diana and Elisa Giovannetti",
year = "2019",
month = "1",
day = "1",
doi = "10.21873/anticanres.13509",
language = "English",
volume = "39",
pages = "3615--3620",
journal = "Anticancer Research",
issn = "0250-7005",
publisher = "International Institute of Anticancer Research",
number = "7",

}

Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole Derivatives against Pancreatic Cancer Cells*. / Li Petri, Giovanna; Cascioferro, Stella; el Hassouni, Btissame; Carbone, Daniela; Parrino, Barbara; Cirrincione, Girolamo; Peters, Godefridus J.; Diana, Patrizia; Giovannetti, Elisa.

In: Anticancer Research, Vol. 39, No. 7, 01.01.2019, p. 3615-3620.

Research output: Contribution to journalArticleAcademicpeer-review

TY - JOUR

T1 - Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole Derivatives against Pancreatic Cancer Cells*

AU - Li Petri, Giovanna

AU - Cascioferro, Stella

AU - el Hassouni, Btissame

AU - Carbone, Daniela

AU - Parrino, Barbara

AU - Cirrincione, Girolamo

AU - Peters, Godefridus J.

AU - Diana, Patrizia

AU - Giovannetti, Elisa

PY - 2019/1/1

Y1 - 2019/1/1

N2 - Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds (1a-g) were submitted to National Cancer Institute (NCI). Remarkably, compound 1g showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory concentration of between 1.67 and 10.3 μM. Further studies showed antiproliferative activity of 1a-g and of three additional compounds 1h, 1i and 1l, with different substituents on the indole nucleus and phenyl ring, against three pancreatic cancer cell lines. In particular, derivatives 1g and 1h inhibited both proliferation and migration of SUIT-2 cells at concentrations lower than 10 μM. In conclusion, new indole derivatives are characterized by in vitro antitumor activity, supporting future mechanistic studies.

AB - Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds (1a-g) were submitted to National Cancer Institute (NCI). Remarkably, compound 1g showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory concentration of between 1.67 and 10.3 μM. Further studies showed antiproliferative activity of 1a-g and of three additional compounds 1h, 1i and 1l, with different substituents on the indole nucleus and phenyl ring, against three pancreatic cancer cell lines. In particular, derivatives 1g and 1h inhibited both proliferation and migration of SUIT-2 cells at concentrations lower than 10 μM. In conclusion, new indole derivatives are characterized by in vitro antitumor activity, supporting future mechanistic studies.

UR - https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85068258278&origin=inward

UR - https://www.ncbi.nlm.nih.gov/pubmed/31262887

U2 - 10.21873/anticanres.13509

DO - 10.21873/anticanres.13509

M3 - Article

VL - 39

SP - 3615

EP - 3620

JO - Anticancer Research

JF - Anticancer Research

SN - 0250-7005

IS - 7

ER -