Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity
Research output: Contribution to journal › Journal article › Research › peer-review
Standard
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 journal › Journal article › Research › peer-review
Harvard
APA
Vancouver
Author
Bibtex
}
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