Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against …

B Zhou, H Li, Z Cui, D Li, H Geng, J Gao… - European Journal of …, 2020 - Elsevier
… Interestingly, the above SAR of 8 for AChE is very similar to that of 2-aryl-β-carbolin-2-ium
salts … In fact, 8 can be considered as simple analogues of 2-aryl-β-carbolin-2-niums [24]. …

DYRK1A inhibitors for disease therapy: current status and perspectives

T Liu, Y Wang, J Wang, C Ren, H Chen… - European journal of …, 2022 - Elsevier
… DYRK1A is involved in multiple biological functions. For … Last but not least, new
strategies are being developed for in … Some investigators conducted SAR studies on …

Synthesis and biological validation of a harmine-based, central nervous system (CNS)-avoidant, selective, human β-cell regenerative dual-specificity tyrosine …

K Kumar, P Wang, J Wilson, V Zlatanic… - Journal of medicinal …, 2020 - ACS Publications
strategy to investigate structure–activity relationships of harmine analogs for both DYRK1A
activity and … In conclusion, through extensive SAR studies and biological characterization, we …

Aza-Annulation of 1,2,3,4-Tetrahydro-β-carboline Derived Enaminones and Nitroenamines: Synthesis of Functionalized Indolizino[8,7-b]indoles, Pyrido[1,2-a:3,4-b′]diindoles …

A Avadhani, P Iniyavan, A Acharya, V Gautam… - ACS …, 2019 - ACS Publications
… We next extended our aza-annulation strategy for the synthesis … (16) Fascaplysin displays
a broad range of biological activities, … with potential biological activity employing this protocol. …

Diabetic kinome inhibitors—A new opportunity for β-cells restoration

B Pucelik, A Barzowska, JM Dąbrowski… - International Journal of …, 2021 - mdpi.com
… , 4-(7-methoxy-1-methyl-β-carbolin-9-yl)butanamide proved to be the … SAR studies on the
aminopyrazine scaffold targeted the … , biological activity with future direction of development are …

Structure-based discovery of ABCG2 inhibitors: a homology protein-based pharmacophore modeling and molecular docking approach

MT Le, VN Hoang, DN Nguyen, THL Bui, TV Phan… - Molecules, 2021 - mdpi.com
… As the case of tetrahydroxy-β-carbolin derivative, … biological activity test of tetrahydro-β-carbolin
group when ethylated -NH- group on this molecule, the biological activity

Design, synthesis, and antifungal evaluation of neocryptolepine derivatives against phytopathogenic fungi

JK Zhu, JM Gao, CJ Yang, XF Shang… - Journal of agricultural …, 2020 - ACS Publications
… Given the broad pharmacological activities of neocryptolepine, … for further structural modification
and SAR development. … Meanwhile, this study also offered a strategy to achieve highly …

DNA related enzymes as molecular targets for antiviral and antitumoral chemotherapy. A natural overview of the current perspectives

HA Garro, CR Pungitore - Current Drug Targets, 2019 - ingentaconnect.com
activity in a specific manner [8]. Consequently, some proteins can become true molecular
targets and then develop certain pharmacological action. … allow the development of new leads, …

Design, Synthesis and Anticancer Activity of Β-Carboline Based Pseudo-Natural Products by Inhibiting Akt/Mtor Signaling Pathway

L Lv, K Song, Y Xiao, J Zheng, W Zhang, L Li… - Mtor Signaling … - papers.ssrn.com
… sensible and rational design strategy in recent years, providing … The structure-activity
relationship (SAR) against A549 is … molecules for exploring relative biological activity and ability to …

Uncovering the relationship between hepatocellular carcinoma and compounds belonging to Simaroubaceae using a network pharmacology approach and molecular …

M Wen, GZ Sen, H Pei, D Xin - Computational Toxicology, 2021 - Elsevier
… D (PA47-a), β-carbolin-1-yl3-(4, 8-dimethoxy-β-carbolin-1-yl)-1-… Network pharmacology is a
new drug discovery strategy … Another important aspect is highlighted by this SAR study deals …