Recent Developments on Synthesis Strategies, SAR Studies and Biological Activities of β-Carboline Derivatives – An Update

Abinaya, R.; Srinath, Santhanam; Soundarya, S.; Sridhar, R.; Balasubramaniam, K. K.; Baskar, Baburaj

doi:10.1016/j.molstruc.2022.132750

Cited by 12 publications

(3 citation statements)

References 250 publications

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“…Carbolines are made up of indole ring and flexible piperidine or pyridine ring and thus may function as both H-bond donor and H-bond acceptor in the drug design approaches. [1] According to their ABC skeleton demonstrated in Figure 1, carbolines are classified into α-, β-, γ-, and δcarbolines. [2] β-Carboline scaffold is distributed widely in nature.…”

Section: Introductionmentioning

confidence: 99%

The Progress in Pictet‐Spengler β‐Carboline Synthesis under Green Conditions

Mousa,

Adly,

Mahmoud

et al. 2024

ChemistrySelect

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Abstractβ‐Carboline ring is widely distributed in nature and several β‐carboline alkaloids were extracted from marine creatures, bacteria, fungi, food stuffs, plants, and mammals. Synthetic β‐carbolines derivatives were reported to exhibit various biological activities. This review highlighted the recent progress achieved in the last decade in the Pictet‐Spengler synthesis of β‐carboline derivatives with a special focus on the green methods and green catalysts used for the synthesis.

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Section: Introductionmentioning

confidence: 99%

The Progress in Pictet‐Spengler β‐Carboline Synthesis under Green Conditions

Mousa,

Adly,

Mahmoud

et al. 2024

ChemistrySelect

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“…The β-carboline ring is present in many naturally occurring alkaloids with variable biological activities such as anticancer, antimicrobial, anti-Alzheimer, antimalarial, anti-inflammatory, antihypertensive, analgesic, and vasorelaxant activities. − There is a wide interest in the development of novel synthetic approaches, , especially green methods for the preparation of β-carboline derivatives . The green methods used for the synthesis of β-carbolines include the use of microwave , and ultrasonic irradiation, as well as the use of various types of catalysts including heterogeneous, organometallic, , inorganic salts, organic, , natural, , and enzymatic catalysis .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Tetrahydro-β-carboline Derivatives under Electrochemical Conditions in Deep Eutectic Solvents

Mousa,

Adly,

Mahmoud

et al. 2024

ACS Omega

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In this work, a novel, green, and atom-efficient method for the synthesis of tetrahydro-β-carboline derivatives using electrochemistry (EC) in deep eutectic solvents (DESs) was reported. The EC reaction conditions were optimized to achieve the highest yield. The experimental design was also optimized to perform the reaction in a two-step, one-pot reaction, thereby the time, workup procedure, and solvents needed were all reduced. The new approach achieved our strategy as EC served to decrease the time of reaction, eliminate the use of hazardous catalysts, and lower the energy required for the synthesis of the targeted compounds. On the other side, DESs were used as catalysts, in situ electrolytes, and noninflammable green solvents. The scope of the reaction was investigated using different aromatic aldehydes. Finally, the scalability of the reaction was investigated using a gram-scale reaction that afforded the product in an excellent yield.

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“…In the past decade, many indole derivatives have been identified as potential Mcl-1 inhibitors . β-Carbolines are a class of natural and synthetic indole heterocyclic alkaloids with various biological activities. − Fesik’s group discovered a β-carboline scaffold that can interact with Mcl-1 protein using the NMR-based screening of 13,824 compounds . Up to now, a series of metal complexes with β-carboline ligands have been developed as anticancer agents, including Re(I), Ag(I), Cu(II), Zn(II), Ru(II), Ni(II), Co(II), Ir(III), Pt(II) complexes .…”

Section: Introductionmentioning

confidence: 99%

Platinum-Based Mcl-1 Inhibitor Targeting Mitochondria Achieves Enhanced Antitumor Activity as a Single Agent or in Combination with ABT-199

Lü

et al. 2023

J. Med. Chem.

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Discovery of small molecule inhibitors targeting Mcl-1 (Myeloid cell leukemia 1) confronts many challenges. Based on the fact that Mcl-1 is mainly localized in mitochondria, we propose a new strategy of targeting mitochondria to improve the binding efficiency of Mcl-1 inhibitors. We report the discovery of complex 9, the first mitochondrial targeting platinum-based inhibitor of Mcl-1, which selectively binds to Mcl-1 with high binding affinity. Complex 9 was mainly concentrated in the mitochondria of tumor cells which led to an enhanced antitumor efficacy. Complex 9 induced Bax/Bak-dependent apoptosis in LP-1 cells and synergized with ABT-199 to kill ABT-199 resistant cells in multiple cancer models. Complex 9 was effective and tolerable as a single agent or in combination with ABT-199 in mouse models. This research work demonstrated that developing mitochondria-targeting Mcl-1 inhibitors is a new potentially efficient strategy for tumor therapy.

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Recent Developments on Synthesis Strategies, SAR Studies and Biological Activities of β-Carboline Derivatives – An Update

Cited by 12 publications

References 250 publications

The Progress in Pictet‐Spengler β‐Carboline Synthesis under Green Conditions

The Progress in Pictet‐Spengler β‐Carboline Synthesis under Green Conditions

Synthesis of Tetrahydro-β-carboline Derivatives under Electrochemical Conditions in Deep Eutectic Solvents

Platinum-Based Mcl-1 Inhibitor Targeting Mitochondria Achieves Enhanced Antitumor Activity as a Single Agent or in Combination with ABT-199

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