Tert-butyl Group bearing Murrayanine-chalcone Produced Noteworthy Anti-proliferative Activity against Breast Cancer Cell Line

Authors

  • Debarshi Kar Mahapatra Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur, Maharashtra, India.
  • Ruchi S Shivhare Department of Pharmaceutical Chemistry, Kamla Nehru College of Pharmacy, Nagpur, Maharashtra, India.
  • Pranesh Kumar Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University (A Central University), Lucknow, Uttar Pradesh, India.

Keywords:

Anti-cancer, Anti-proliferative, Anti-oxidant, Chalcone, Murrayanine, Tert-butyl

Abstract

Cancer is the deadliest disease after cardiovascular diseases and is expected to increase by nearly twice in number by the end of the year 2050. It is rapidly progressing and a majority of the well-known anticancer drugs are in the path of getting resistant. In our previous study, we had rationally designed a hybrid molecule which comprised of murrayanine (carbazole moiety), chalcone, and tert-butyl group, and predicted that that hybridization will lead to enhanced synergistic anti-oxidant activity. The free-radical scavenging screening by DPPH assay was found to be absolutely correct and the chalcone demonstrated nearly analogous scavenging of the reactive species with that of ascorbic acid. Likewise, due to a close association of freeradical species and cancer, the fabricated prop-2-ene-1-one compound having marvelous anti-oxidant activity was screened for anti-proliferative activity against breast cancer MCF-7 cell line using SRB assay and was expected to produce better results than the individual components. The anti-cancer SRB assay of the hybrid compound demonstrated a remarkable anti-proliferative activity with an IC50 value of 19.67 ?M. The present research will surely motivate the researchers in further developing better chalcone based anti-cancer drugs along with inspiration towards the pharmaceutical product development.

References

1. Mahapatra DK, Bharti SK. Handbook of Research on
Medicinal Chemistry: Innovations and Methodologies.
Apple Academic Press, New Jersey. 2017.
2. Mahapatra DK, Bharti SK. Drug Design. Tara Publications
Private Limited, New Delhi. 2016.3. Shivhare RS, Mahapatra DK, Nair RR et al. Schiff’s base
derivatives of murrayanine demonstrated enhanced
anti-oxidant activity than its parent moiety. Indian J
Pharm Edu Res 2016; 50(4): 9-15.
4. Mahapatra DK, Shivhare RS. Synthesizing an antioxidant
principle 2-(((1-methoxy-9H-carbazol-3-
yl)methylene)amino)isoindoline-1,3-dione from
N-aminophthalimide and murrayanine. Inventi Med
Chem 2017; (4): 1-3.
5. Mahapatra DK, Dadure KM, Shivhare RS. MCF-7 cell
line screening of some uracil containing murrayanine
based (thio)-semicarbazide hybrids. Innovat Int J Med
Pharm Sci 2018; 3(5): 14-6.
6. Mahapatra DK, Das D, Shivhare RS. Substituted
thiazole linked murrayanine-Schiff’s base derivatives
as potential anti-breast cancer candidates: Future
EGFR kinase inhibitors. Int J Pharm Sci Drug Res 2017;
9(3): 139-44.
7. Bashir M, Bano A, Ijaz AS, Chaudhary BA. Recent
developments and biological activities of n-substituted
carbazole derivatives: a review. Molecules 2015; 20(8):
13496-517.
8. Mahapatra DK, Bharti SK, Asati V. Anti-cancer chalcones:
structural and molecular targets perspectives. Eur J
Med Chem 2015; 98: 69-114.
9. Murakami Y, Kawata A, Katayama T et al. Antiinflammatory
Activity of the Artificial Antioxidants
2-Tert-butyl-4-methoxyphenol (BHA), 2, 6-Di-tert-butyl-
4-methylphenol (BHT) and 2, 4, 6-Tri-tert-butylphenol
(TBP), and their various combinations. In vivo 2015;
29(2): 197-206.
10. Mahapatra DK, Shivhare RS. Substituting tert-butyl
group on murrayanine-chalcone scaffold produced
tremendously high anti-oxidant activity than the
individual components. Int J Anal Med Chem 2018;
1(1): 1-5.
11. Mahapatra DK, Shivhare RS, Borkar SS. Tert-butyl Group
Substitution in the Ring-B of murrayanine-chalcone
leads to higher expression of edema reduction.
(Communicated).
12. Padole CD, Amdare MD, Jogdand KR et al. Discovery of
4-methyl-2-oxo-2H-chromen-7-yl-2-benzamidoacetate
as anti-proliferative agent. Int J Ayur Pharm Chem
2018; 8(1): 62-8.

Downloads

Published

2018-12-26

Issue

Vol. 1 No. 3&4 (2018): Journal of Advanced Research in BioChemistry and Pharmacology

Section

Research Article

License

We, the undersigned, give an undertaking to the following effect with regard to our article entitled
“_______________________________________________________________________________________________________________________________________________________________________________
________________________________________________________________________________” submitted for publication in (Journal title)________________________________________________ _______________________________________________________Vol.________, Year _________:-

1. The article mentioned above has not been published or submitted to or accepted for publication in any form, in any other journal.

2. We also vouchsafe that the authorship of this article will not be contested by anyone whose name(s) is/are not listed by us here.

3. I/We declare that I/We contributed significantly towards the research study i.e., (a) conception, design and/or analysis and interpretation of data and to (b) drafting the article or revising it critically for important intellectual content and on (c) final approval of the version to be published.

4. I/We hereby acknowledge ADRs conflict of interest policy requirement to scrupulously avoid direct and indirect conflicts of interest and, accordingly, hereby agree to promptly inform the editor or editor's designee of any business, commercial, or other proprietary support, relationships, or interests that I/We may have which relate directly or indirectly to the subject of the work.

5. I/We also agree to the authorship of the article in the following sequence:-

Authors' Names (in sequence) Signature of Authors
1. _____________________________________ _____________________________________
2. _____________________________________ _____________________________________
3. _____________________________________ _____________________________________
4. _____________________________________ _____________________________________
5. _____________________________________ _____________________________________
6. _____________________________________ _____________________________________
7. _____________________________________ _____________________________________
8. _____________________________________ _____________________________________

Important

(I). All the authors are required to sign independently in this form in the sequence given above. In case an author has left the institution/ country and whose whereabouts are not known, the senior author may sign on his/ her behalf taking the responsibility.

(ii). No addition/ deletion/ or any change in the sequence of the authorship will be permissible at a later stage, without valid reasons and permission of the Editor.

(iii). If the authorship is contested at any stage, the article will be either returned or will not be
processed for publication till the issue is solved.