Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity

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Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity. / Kankala, Shravankumar; Rama, Koteshwar Rao; Kesari, Chekrapani; Bjorkling, Fredrik; Nerella, Srinivas; Gundepaka, Prasad; Guguloth, Hanmanthu; Thota, Niranjan.

In: Synthetic Communications, Vol. 50, No. 19, 2020, p. 2997-3006.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Kankala, S, Rama, KR, Kesari, C, Bjorkling, F, Nerella, S, Gundepaka, P, Guguloth, H & Thota, N 2020, 'Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity', Synthetic Communications, vol. 50, no. 19, pp. 2997-3006. https://doi.org/10.1080/00397911.2020.1791341

APA

Kankala, S., Rama, K. R., Kesari, C., Bjorkling, F., Nerella, S., Gundepaka, P., Guguloth, H., & Thota, N. (2020). Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity. Synthetic Communications, 50(19), 2997-3006. https://doi.org/10.1080/00397911.2020.1791341

Vancouver

Kankala S, Rama KR, Kesari C, Bjorkling F, Nerella S, Gundepaka P et al. Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity. Synthetic Communications. 2020;50(19):2997-3006. https://doi.org/10.1080/00397911.2020.1791341

Author

Kankala, Shravankumar ; Rama, Koteshwar Rao ; Kesari, Chekrapani ; Bjorkling, Fredrik ; Nerella, Srinivas ; Gundepaka, Prasad ; Guguloth, Hanmanthu ; Thota, Niranjan. / Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity. In: Synthetic Communications. 2020 ; Vol. 50, No. 19. pp. 2997-3006.

Bibtex

@article{9ba062fbc3b84a7093b33e0b819a755e,
title = "Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity",
abstract = "A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed byin situformed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated forin vitroanticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds,11c,11e,11j, and11k, showed growth inhibition (low mu M) comparable with the standard drug cisplatin, providing a preliminary structure-activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.",
keywords = "Fluorophenylpyrazole-picolinamide, cross-coupling, palladium-N-heterocyclic carbenes, anticancer activity, ONE-POT SYNTHESIS, BIOLOGICAL EVALUATION, PYRAZOLE DERIVATIVES, ANTITUMOR AGENTS, HYBRIDS, DESIGN, HETEROCYCLES, CANCER",
author = "Shravankumar Kankala and Rama, {Koteshwar Rao} and Chekrapani Kesari and Fredrik Bjorkling and Srinivas Nerella and Prasad Gundepaka and Hanmanthu Guguloth and Niranjan Thota",
year = "2020",
doi = "10.1080/00397911.2020.1791341",
language = "English",
volume = "50",
pages = "2997--3006",
journal = "Synthetic Communications",
issn = "0039-7911",
publisher = "Taylor & Francis",
number = "19",

}

RIS

TY - JOUR

T1 - Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity

AU - Kankala, Shravankumar

AU - Rama, Koteshwar Rao

AU - Kesari, Chekrapani

AU - Bjorkling, Fredrik

AU - Nerella, Srinivas

AU - Gundepaka, Prasad

AU - Guguloth, Hanmanthu

AU - Thota, Niranjan

PY - 2020

Y1 - 2020

N2 - A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed byin situformed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated forin vitroanticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds,11c,11e,11j, and11k, showed growth inhibition (low mu M) comparable with the standard drug cisplatin, providing a preliminary structure-activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.

AB - A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed byin situformed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated forin vitroanticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds,11c,11e,11j, and11k, showed growth inhibition (low mu M) comparable with the standard drug cisplatin, providing a preliminary structure-activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.

KW - Fluorophenylpyrazole-picolinamide

KW - cross-coupling

KW - palladium-N-heterocyclic carbenes

KW - anticancer activity

KW - ONE-POT SYNTHESIS

KW - BIOLOGICAL EVALUATION

KW - PYRAZOLE DERIVATIVES

KW - ANTITUMOR AGENTS

KW - HYBRIDS

KW - DESIGN

KW - HETEROCYCLES

KW - CANCER

U2 - 10.1080/00397911.2020.1791341

DO - 10.1080/00397911.2020.1791341

M3 - Journal article

VL - 50

SP - 2997

EP - 3006

JO - Synthetic Communications

JF - Synthetic Communications

SN - 0039-7911

IS - 19

ER -

ID: 248193880