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Tanatorn Khotavivattanal. Synthesis of benzofuropyridine analogues for potential oncologic drug applications. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2023.
Synthesis of benzofuropyridine analogues for potential oncologic drug applications
Name: Ereje, Reymark
Organization :
Chulalongkom University. Faculty of Science
Organization :
Chulalongkom University. Faculty of Science
Name: Somsak Pianwanit
Organization :
Chulalongkom University. Faculty of Science
Name: Jantana Yahuafait
Organization :
Chulalongkom University. Faculty of Science
Name: Chanat Aonbangkhen
Organization :
Chulalongkom University. Faculty of Science
Name: Tanatorn Khotavivattanal
Organization :
Chulalongkom University. Faculty of Science
Email :
tanatorn.k@chula.ac.th
keyword:
Benzofuropyridines
LCSH:
Benzoic acid
-- Synthesis
LCSH:
Drug development
LCSH:
Antineoplastic agents
Abstract:
Cancer is a disease characterized by abnormal cell proliferation, with its current therapies limited due to
cytotoxicity to normal cells. Benzofuropyridines (BFP) are a class of tricyclic small molecules derivatized from the
original a-carboline core strnucture mainly used for cytostatic cancer regimen. Although reported with anticancer activity,
the potential of BFP and its analogues has not been fully elucidated. Herein, a series of benzylated 2,6-
dihydroxybenzofuropyridine (2,6-dhBFP) derivatives were synthesized and cytotoxicity assay against three cancer cell
lines was performed. The results revealed that some analogues showed moderate inhibition at 50 JM ranging from 45-
65% in SH-SY5Y (neuroblastoma) and 45-62% in HepG2 (hepatocarcinoma) cells while the 2-hydroxy derivatives 5a
and 5c exhibited promising ICso at micromolar range of 36 and 14 uM respectively, with significantly improved activity
compared to the underivatized 2,6-dhBFP at 150 JM in KB (oral epidermoid) cancer cells. Moreover, molecular docking
study was conducted using cyclin-dependent kinase 5 (CDK5) showing enhanced binding affinity for all analogues and
top value of -9.45 kcalmol as compared to -7.69 kcal/mol for 2,6-dhBFP and -8.39 kcal mol for roscovitine, a known
CDK inhibitor. Overall, this study provided substantial insights on the potential of the BFP moiety as candidate for
future cancer therapies.
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2023
Modified:
2023-07-12
Issued:
2023-07-12
บทความ/Article
application/pdf
BibliograpyCitation :
In Mae Fah Luang University. School of Science. The Pure and Applied Chemistry International Conference 2023 (PACCON 2023) (pp.753-758). Chiang Rai : Mae Fah Luang University
eng
©copyrights King Mongkut's University of Technology North Bangkok
RightsAccess:
ใช้เวลา
0.023892 วินาที
Ereje, Reymark
| Title | Contributor | Type |
|---|---|---|
| Synthesis of benzofuropyridine analogues for potential oncologic drug applications
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ereje, Reymark;Theeranuch Jaroenchuensiri;Somsak Pianwanit;Jantana Yahuafait;Chanat Aonbangkhen;Tanatorn Khotavivattanal | บทความ/Article |
Theeranuch Jaroenchuensiri
| Title | Contributor | Type |
|---|---|---|
| Synthesis of benzofuropyridine analogues for potential oncologic drug applications
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ereje, Reymark;Theeranuch Jaroenchuensiri;Somsak Pianwanit;Jantana Yahuafait;Chanat Aonbangkhen;Tanatorn Khotavivattanal | บทความ/Article |
Somsak Pianwanit
| Title | Contributor | Type |
|---|---|---|
| Synthesis of benzofuropyridine analogues for potential oncologic drug applications
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ereje, Reymark;Theeranuch Jaroenchuensiri;Somsak Pianwanit;Jantana Yahuafait;Chanat Aonbangkhen;Tanatorn Khotavivattanal | บทความ/Article |
Jantana Yahuafait
| Title | Contributor | Type |
|---|---|---|
| Synthesis of benzofuropyridine analogues for potential oncologic drug applications
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ereje, Reymark;Theeranuch Jaroenchuensiri;Somsak Pianwanit;Jantana Yahuafait;Chanat Aonbangkhen;Tanatorn Khotavivattanal | บทความ/Article |
Chanat Aonbangkhen
| Title | Contributor | Type |
|---|---|---|
| Synthesis of benzofuropyridine analogues for potential oncologic drug applications
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ereje, Reymark;Theeranuch Jaroenchuensiri;Somsak Pianwanit;Jantana Yahuafait;Chanat Aonbangkhen;Tanatorn Khotavivattanal | บทความ/Article |
Tanatorn Khotavivattanal
| Title | Contributor | Type |
|---|---|---|
| Synthesis of benzofuropyridine analogues for potential oncologic drug applications
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ereje, Reymark;Theeranuch Jaroenchuensiri;Somsak Pianwanit;Jantana Yahuafait;Chanat Aonbangkhen;Tanatorn Khotavivattanal | บทความ/Article | |
| Analogs of lapatinib from its fragmented core structure inhibit SARS-CoV-2 main proteases
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Ayomide Adediiil;Akeanan Sroithongmoon;Siwaporn Boonyasuppayakomn;Aphinya Suroengrit;Patcharin Wilasluck;Peerapon Deetanya;Kittikhun Wangkanont;Thanyada Rungrotmongkols;Kamonpan Sanachai;Tanatorn Khotavivattanal | บทความ/Article |