Tag: 100-200

Synthesis and evaluation of new isatin derivatives for cytotoxic activity was written by Priyanka, K. Blessi;Manasa, C.;Sammaiah, G.. And the article was included in World Journal of Pharmacy and Pharmaceutical Sciences in 2014.Computed Properties of C8H4N2O4 This article mentions the following:

A series of semicarbazones I (R = 5-Br, 7-NO₂, 5-CH₃, etc.) was synthesized and screened for their cytotoxic activity by MTT assay method. All synthesized compounds I exhibited significant cytotoxicity in a concentration-dependent manner. The IC₅₀ values of all test compounds I were found to be between 19.27 and 52.45 mM for MCF-7 cell lines and between 14.10 and 31.6 mM for HeLa cell lines. All the synthesized compounds have shown moderate antioxidant activity. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Computed Properties of C8H4N2O4).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Computed Properties of C8H4N2O4

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Studies on the chemistry of isoindoles and isoindolenines. XXVII. 3-Alkoxy-1H-isoindoles: syntheses and properties was written by Hennige, Hans;Kreher, Richard P.;Konrad, Michael;Jelitto, Frank. And the article was included in Chemische Berichte in 1988.Recommanded Product: 6-Nitroisoindolin-1-one This article mentions the following:

3-Alkoxy-1H-isoindoles I (R = H, 5-O₂N, 6-MeO, 5,6-Me₂, 4,7-Me₂, 5,6-Cl₂, 4,5,6,7-Cl₄; R¹ = Me, Et) were prepared from substituted 2,3-dihydro-1H-isoindol-1-ones by regiospecific O-alkylation with trialkyloxonium tetrafluoroborates or with trifluoromethanesulfonates, and subsequent NH deprotonation. According to the spectroscopic properties, the semicyclic alkyl imidates I exist exclusively in the benzenoid 1H structure; the tautomeric o-quinonoid 2H structure cannot be detected by spectroscopic means. In the experiment, the researchers used many compounds, for example, 6-Nitroisoindolin-1-one (cas: 110568-64-4Recommanded Product: 6-Nitroisoindolin-1-one).

6-Nitroisoindolin-1-one (cas: 110568-64-4) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Recommanded Product: 6-Nitroisoindolin-1-one

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Alpha-ethyltryptamines as dual dopamine-serotonin releasers was written by Blough, Bruce E.;Landavazo, Antonio;Partilla, John S.;Decker, Ann M.;Page, Kevin M.;Baumann, Michael H.;Rothman, Richard B.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Computed Properties of C9H6ClNO This article mentions the following:

The dopamine (DA), serotonin (5-HT), and norepinephrine (NE) transporter releasing activity and serotonin-2A (5-HT_2A) receptor agonist activity of a series of substituted tryptamines are reported. Three compounds, 7b, (+)-7d and 7f, were found to be potent dual DA/5-HT releasers and were >10-fold less potent as NE releasers. Addnl., these compounds had different activity profiles at the 5-HT_2A receptor. The unique combination of dual DA/5-HT releasing activity and 5-HT_2A receptor activity suggests that these compounds could represent a new class of neurotransmitter releasers with therapeutic potential. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Computed Properties of C9H6ClNO).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Computed Properties of C9H6ClNO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and antitumor activity of 5伪, 8伪-peroxide steroid derivatives containing dihydrazone unit was written by Bu, Ming;You, Dan;Zhang, Song;Chen, Zhe. And the article was included in Huaxue Shiji in 2019.Formula: C9H6ClNO This article mentions the following:

Using dehydroepiandrosterone (DHEA) as staring material, five steroidal endoperoxide derivatives with different indole side chain structures had been synthesized, and the structures were confirmed by MS, ¹HNMR and ¹³CNMR. The antiproliferative activity was evaluated against human liver carcinoma cells (HepG2), human breast cancer cells (MCF-7) and normal kidney epithelial cells (293 T). The results showed that 5伪,8伪-epidioxy-17-(5-fluoro-indol-3-ylmethylene) hydrazonoandrostan-3尾-ol and 5伪,8伪-epidioxy-17-(5-chloro-indol-3-ylmethylene) hydrazonoandrostan-3尾-ol had significant inhibitory activity to the tested cancer cells. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Formula: C9H6ClNO).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Formula: C9H6ClNO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

3-Benzamides and 3,4,5-trimethoxyphenyl amines as calcium channel blockers was written by Kang, Bohee;Oh, Jung Ae;Lee, Jee Youn;Rhim, Hyewhon;Yune, Tae Young;Park Choo, Hea-Young. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Application In Synthesis of 5-Chloroindole-3-carboxaldehyde This article mentions the following:

T- and N-type calcium channels have known for relating to therapy of neuropathic pain which is chronic, debilitating pain state. Neuropathic pain is caused by damage of the somatosensory system. It may be associated with abnormal sensations and pain produced by normally non-painful stimuli (allodynia). Neuropathic pain is very difficult to treat, and only some 40-60% of patients achieve partial relief. For a neuropathic pain therapy, anticonvulsant like Lamotrigine, Carbamazepine and a topical anesthetic such as Lidocaine are used. We synthesized 15 novel amine derivatives and evaluated their activities against T-type and N-type calcium channels by whole-cell patch clamp recording on HEK293 cells. Among the tested compounds, compound 10 showed good inhibitory activity for both T-type and N-type calcium channels with the IC₅₀ value of 1.9 渭M and 4.3 渭M, resp. Compound 10 also showed good analgesic activity on rat spinal cord injury model. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Application In Synthesis of 5-Chloroindole-3-carboxaldehyde).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Application In Synthesis of 5-Chloroindole-3-carboxaldehyde

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

The synthesis of symmetrical 3,3-Disubstituted oxindoles by phosphine-catalyzed 纬/纬-addition of oxindoles with allenoates was written by Zhang, Ji-Quan;Li, Shu-Min;Wu, Chun-Feng;Wang, Xing-Lan;Wu, Ting-Ting;Du, Yao;Yang, Yuan-Yong;Fan, Ling-Ling;Dong, Yong-Xi;Wang, Jian-Ta;Tang, Lei. And the article was included in Catalysis Communications in 2020.Product Details of 774-47-0 This article mentions the following:

A phosphine-catalyzed 纬/纬-addition of oxindoles I (R¹ = H, 5,7-F₂, 6-OMe, 5-Cl, etc.; R² = Me, Boc, Bn, Ph; R³ = H, R⁴ = H, Ph) and II (R² = acetyl, Boc; R³ = H) with allenoates as Et buta-2,3-dienoate, Me buta-2,3-dienoate, benzyl buta-2,3-dienoate has been developed that enables the efficient synthesis of highly functionalized sym. 3,3-disubstituted oxindoles I (R³ = (2E)-4-ethoxy-4-oxobut-2-en-1-yl, (2E)-4-methoxy-4-oxobut-2-en-1-yl, (2E)-4-benzyloxy-4-oxobut-2-en-1-yl; R⁴ = (2E)-4-ethoxy-4-oxobut-2-en-1-yl, (2E)-4-methoxy-4-oxobut-2-en-1-yl, (2E)-4-benzyloxy-4-oxobut-2-en-1-yl, Ph), II (R³ = (2E)-4-ethoxy-4-oxobut-2-en-1-yl). This protocol features mild reaction conditions and wide functional group tolerance and affords corresponding addition products in good to excellent yields. Besides, have also been investigated the biol. utility of the typical 3,3-disubstituted oxindoles against nine phytopathogenic fungi, and I (R¹ = H, R² = Me, R³ = R⁴ = (2E)-4-ethoxy-4-oxobut-2-en-1-yl; R¹ = 5-Br, R² = Me, R³ = R⁴ = (2E)-4-ethoxy-4-oxobut-2-en-1-yl) and exhibited promising antifungal activities. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0Product Details of 774-47-0).

5,6-Difluoroindoline-2,3-dione (cas: 774-47-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Product Details of 774-47-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Antioxidant, Cytotoxic Activities, and Structure-Activity Relationship of Gallic Acid-based Indole Derivatives was written by Khaledi, Hamid;Alhadi, Abeer A.;Yehye, Wagee A.;Ali, Hapipah Mohd.;Abdulla, Mahmood A.;Hassandarvish, Pouya. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2011.Application of 827-01-0 This article mentions the following:

A new series of gallic hydrazones containing an indole moiety was synthesized through the reaction of gallic hydrazide and different indole carboxaldehydes. Their antioxidant activities were determined on DPPH radical scavenging and inhibition of lipid peroxidation The in-vitro cytotoxic activities of the compounds were evaluated against HCT-116 (human colon cancer cell line) and MCF-7 (estrogen-dependent human breast cancer cell line) by the MTT method. An attempt to correlate the biol. results with their structural characteristics has been done. A limited pos. structure activity relationship was found between cytotoxic and antioxidant activities. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Application of 827-01-0).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application of 827-01-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An improved synthesis, characterization and bioevalution of Schiff base containing benzimidazole moiety catalyzed by methane sulfonic acid was written by Krishna Rao, N.;Surendra, Babu M. S.;Ramana, N.;Tentu, Nageswara Rao;Basaveswara Rao, M. V.;Karri, Apparao. And the article was included in Pharma Chemica in 2017.Related Products of 827-01-0 This article mentions the following:

An improved process for the synthesis for some novel Schiff bases I [R = H, Me, Cl, etc.] by the reaction of 2-amino benzimidazole with 5-substituted indole-3-carbaldehyde using methane sulfonic acid as catalyst under solvent free conditions at room temp was reported. The intermediate moiety 2-aminobenzimidazole could be synthesized by reacting o-phenylene diamine with cyanobromide in the presence of acid medium. All compounds were screened for their antibacterial activities and compounds I [R = Br, Cl] exhibited high antibacterial activity potential. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Related Products of 827-01-0).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Related Products of 827-01-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Electrosynthesis of (hetero)aryl nitriles from 伪-imino-oxy acids via oxidative decarboxylation/N-O cleavage was written by Lin, Hui-Shan;Chen, Shu-Jun;Huang, Jing-Mei. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2022.Recommanded Product: 5-Chloroindole-3-carboxaldehyde This article mentions the following:

A new method for the synthesis of (hetero)aryl nitriles via iminyl radicals was developed through the electrochem. oxidative decarboxylation of 伪-imino-oxy acids. This protocol provides an efficient approach to nitriles with a broad range of functional-group tolerance under ambient conditions and can be applied for one-pot gram-scale synthesis. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Recommanded Product: 5-Chloroindole-3-carboxaldehyde).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Recommanded Product: 5-Chloroindole-3-carboxaldehyde

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles