Design, synthesis of novel N prenylated indole-3-carbazones and evaluation of in vitro cytotoxicity and 5-LOX inhibition activities

Praveen Choppara; Y.V. Prasad; C.V. Rao; K. Hari Krishna; G. Trimoorthulu; G.U. Maheswara Rao; J. Venkateswara Rao; M.S. Bethu; Y.L.N. Murthy

Arabian Journal of Chemistry (Dec 2019)

Design, synthesis of novel N prenylated indole-3-carbazones and evaluation of in vitro cytotoxicity and 5-LOX inhibition activities

Praveen Choppara,
Y.V. Prasad,
C.V. Rao,
K. Hari Krishna,
G. Trimoorthulu,
G.U. Maheswara Rao,
J. Venkateswara Rao,
M.S. Bethu,
Y.L.N. Murthy

Affiliations

Praveen Choppara: Department of Organic Chemistry, Foods, Drugs & Water, Andhra University, Visakhapatnam 530 003, India
Y.V. Prasad: Department of Organic Chemistry, Foods, Drugs & Water, Andhra University, Visakhapatnam 530 003, India
C.V. Rao: Resaearch & Development Centre, Laila impex, Vijayawada 520 007, India
K. Hari Krishna: Resaearch & Development Centre, Laila impex, Vijayawada 520 007, India
G. Trimoorthulu: Resaearch & Development Centre, Laila impex, Vijayawada 520 007, India
G.U. Maheswara Rao: Resaearch & Development Centre, Laila impex, Vijayawada 520 007, India
J. Venkateswara Rao: Biology Division, Indian Institute of Chemical Technology, Hyderabad 500 007, (AP), India
M.S. Bethu: Biology Division, Indian Institute of Chemical Technology, Hyderabad 500 007, (AP), India
Y.L.N. Murthy: Department of Organic Chemistry, Foods, Drugs & Water, Andhra University, Visakhapatnam 530 003, India; Corresponding author. Tel.: +91 9849229804; fax: +91 891 2713813.

Journal volume & issue: Vol. 12, no. 8
pp. 2328 – 2335

Abstract

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A series of novel N-1 and C-3 substituted indole derivatives (5a–f) were designed, synthesized and evaluated for their cytotoxic properties, viz Brine Shrimp Lethality Bioassay (BSLB) besides 5-Lipoxygenase (5-LOX) inhibitory activities through in vitro assays. Structure Activity Relation (SAR) studies showed that compound 5d with an LC50 of 6.49 μM and 5c with an IC50 of 33.69 μM were found to be interesting for cytotoxicity and 5-LOX inhibitory activity respectively. Keywords: Brine shrimp lethality bioassay, Cytotoxicity, 5-Lipoxygenase inhibition, N prenylated indole-3-carbazones

Published in Arabian Journal of Chemistry

ISSN: 1878-5352 (Print)
Publisher: Elsevier
Country of publisher: Netherlands
LCC subjects: Science: Chemistry
Website: http://www.journals.elsevier.com/arabian-journal-of-chemistry/

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