Garuda - Garba Rujukan Digital

Bambang Tri Purwanto

Unknown Affiliation

Author-ID : 3511375

Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Chemistry Materials Science & Nanotechnology Medicine & Pharmacology

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1

Analgesic Activity of Acyl-Salicylic Acid Derivatives And In Silico Docking Study For Their Potency As Cyclooxygenase-2 Inhibitors Nuzul Wahyuning Diyah; Anindi Lupita Nasyanska; Bambang Tri Purwanto; Siswandono Siswandono
Berkala Ilmiah Kimia Farmasi Vol. 7 No. 2 (2020): DESEMBER
Publisher : Universitas Airlangga

A series of acyl salicylic acid derivatives were screened to investigate their analgesic activities and their potency as cyclooxygenase-2 (COX-2) inhibitors. Fourteen compounds (BS1–14) were assayed by acetic acid induced writhing test. Their ability for interaction with COX-2 was studied through a docking simulation at the COX-2 active site (PDB. 5IKQ). The results of the analgesic activity test gave 3 compounds that produce ED50< 0.39 mmol/kg body weight, lower than aspirin as a positive control. The compounds BS3 and BS4 showed excellent analgesic activity and the tert-butyl substituted molecule BS3 (O-(4-tert-butylbenzoyl)-salicylic acid analog) showed the highest analgesic activity with ED50 of 0.26 mmol/kg. Based on in silico molecular docking, it is known that almost all of the tested ligands (12 compounds) showed a higher binding affinity for COX-2 than meclofenamic acid which is a COX-2 inhibitory NSAID. The results of in vivo analgesic activity were justified with the outcome of in silico investigation. Molecular docking of acyl-salicylates confirmed in vivo experiments and it was found that BS3 was the most active compound as an analgesic agent and the most potent as a COX-2 inhibitor among the evaluated compounds.a

Sintesis Senyawa N-(2-Klorobenzoil)-N’-Fenilurea dan Uji Aktivitas Anti Kanker Terhadap Sel HeLa Bambang Tri Purwanto
JURNAL ILMU KEFARMASIAN INDONESIA Vol 16 No 2 (2018): JIFI
Publisher : Fakultas Farmasi Universitas Pancasila

Research in the search for cancer drug compounds continue to be developed given the lack of specific anticancer compounds. Some urea derived compounds are also continuously being developed in search of potent anticancer compounds with minimal side effects. In relation to the above, we want to develop an urea derivative of N-phenylurea compound which will be reacted with benzoyl chloride derivative that is 2-chlorobenzoyl chloride so that N-(2-chlorobenzoyl) -N'phenylurea will be obtained. Synthesis of N- (2-chlorobenzoyl) -N'phenylurea was done by modified Schotten-Baumman method, then purity test was performed with thin layer chromatography using 3 different solvents. The next step is structural characterization using UV and IR spectrophotometry method, then 1H-NMR and MS spectrometry, so that the structure of N- (2-chlorobenzoyl) -N'phenylurea will be obtained. An anticancer activity test is performed on HeLa cells using MTT assay method and IC50 value will be obtained. Compounds that have been successfully synthesized are compound of N- (2-chlorobenzoyl) -N'phenylurea, with yield of 80.47% in the form of white needle crystal. The purity test of the N- (2-chlorobenzoyl) -N'phenylurea compound was performed by thin layer chromatography with 3 different solvents (hexan: ethyl acetate: methanol = 2: 3: 1; Hexan: acetone = 4: 2; Hexan: ethylacetate = 4: 2) a single stain is obtained which is different from the Rf value compared to the N-phenylurea origin compound. The Melting Point of the compound is 149oC so it is seen that the compound has been formed and different from the origin compound of N-phenylurea. The anticancer activity test after performed with MTT assay method using HeLa cells line, has an IC50 2100 mg / ml or 8,52 mM for the N- (2-chlorobenzoyl) -N'phenylurea and higher than hydroxy urea as standard compound which has the activity as 7537 mg / ml or 99,10 mM. Conclusion: N- (2-chlorobenzoyl) -N'phenylurea compound has been successfully synthesized and can be further developed as an anticancer compound. Keywords: Synthesis; N-(2-chlorobenzoyl)-N'phenylurea; anticancer activity; HeLa cells.

SINTESIS, UJI AKTIVITAS SITOTOKSIK IN VITRO DAN MOLECULAR DOCKING SENYAWA 1-(4-KLOROBENZOIL)-1,3-DIMETILUREA Dian Agung Pangaribowo; Siswandono Siswandono; Bambang Tri Purwanto
Jurnal Kimia Terapan Indonesia Vol 16, No 1 (2014)
Publisher : Research Center for Chemistry - LIPI

Senyawa 1-(4-klorobenzoil)-1,3-dimetilurea telah dirancang, disintesis, diidentifikasi struktur, dan diuji aktivitas sitotoksik secara in vitro. Simulasi docking dilakukan dengan memposisikan senyawa ke dalam sisi aktif reseptor Checkpoint kinase 1 (Chk1) untuk menentukan model pengikatan ligan reseptor. Sintesis 1-(4-klorobenzoil)-1,3-dimetilurea dilakukan lewat reaksi asilasi antara 1,3-dimetilurea dan 4-klorobenzoil klorida. Kemurnian produk hasil sintesis ditentukan dengan metode Kromatografi Lapis Tipis (KLT).Identifikasi struktur dilakukan dengan spektrofotometer UV, FT-IR dan spektrometer NMR. Hasil uji antiproliferatif menunjukkan bahwa senyawa 1-(4-klorobenzoil)-1,3-dimetilurea memiliki aktivitas sitotoksik terhadap sel HeLa yang lebih baik dibandingkan dengan kontrol positif yaitu hidroksiurea. Senyawa 1-(4-klorobenzoil)-1,3-dimetilurea dengan potensi aktivitas sitotoksik ini dapat menjadi agen antikanker yang potensial.Â Kata kunci: 1-(4-klorobenzoil)-1,3-dimetilurea, molecular docking, sintesis, aktivitas sitotoksik, hidroksiureaÂ A novel 1-(4-chlorobenzoyl)-1,3-dimethylurea has been designed, synthesized, structurally determined, and the in vitro cytotoxic activity was evaluated. Docking simulation was performed to position this compound into the Checkpoint kinase 1 (Chk1) active site to determine the probable binding model. Synthesis of 1-(4-chlorobenzoyl)-1,3-dimethylurea was completed by acylation reaction between 1,3-dimethylurea and 4-chlorobenzoyl chloride. The purity of synthesized product was determined by Thin Layer Chromatography. Structure identification was performed by UV spectrophotometer, FT-IR and NMR spectrometer. Antiproliferative assay result demonstrated that this compound possessed good cytotoxic activity against HeLa cells, which is comparable to the positive control, hydroxyurea. This compound with potent cytotoxic activity might be a potential anticancer agent.Â Keywords: 1-(4-chlorobenzoyl)-1,3-dimethylurea, molecular docking, synthesis, cytotoxic activity

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